向华｜中国药科大学｜学者主页

2026

Optimization of a Second-Generation, Highly Selective Polθ/PARP1 Dual Inhibitor with Improved Pharmacokinetics and Potent Activity against HR-Deficient Tumors

Luyu Ma, Mingzhe Zhong, Yingxuan Chang, Mingjin Luo, Xinyan Liu, Xiaofan Ge, Sitian Xu, Yun Zhang, Ziye Liu, Hua Xiang, Guoshun Luo

Journal of Medicinal Chemistry

DOI

2026

Discovery of an orally bioavailable selenium-containing Polθ inhibitor with a dual mechanism of DNA damage and immune activation for HR-deficient cancers

Luyu Ma, Mingjin Luo, Mingjin Luo, Xiangchi Liu, Jinyue Yang, Jianyu Li, Mingzhe Zhong, Xinyan Liu, Maoxu Xiao, Hua Xiang, Guoshun Luo

European Journal of Medicinal Chemistry

DOI

2026

Approved Steroidal Drugs (2000–2025): A Medicinal Chemistry Perspective

Jiacheng Zhu, Guoshun Luo, Hua Xiang

Journal of Medicinal Chemistry

DOI

2026

The PROTAC milestone: FDA approval of vepdegestrant (ARV-471) for ESR1-mutated breast cancer

Xin Lin, Hua Xiang, Guoshun Luo

Drug Discovery Today

DOI

2026

A patent review of DNA polymerase theta (Polθ) targeted therapies (2019–2025)

Luyu Ma, Mingjin Luo, Hua Xiang, Guoshun Luo

Expert Opinion on Therapeutic Patents

DOI

2026

Lysine-targeted covalent inhibitors: mechanistic advances, pharmacological perspectives and translational challenges

Mingjin Luo, Luyu Ma, Guoshun Luo, Hua Xiang

Biochemical Pharmacology

DOI

2025

Targeted degradation of Werner syndrome helicase (WRN) via ligand-directed covalent hydrophobic tagging

Wenxiang Tao, Jiacheng Zhu, Zixuan Fu, Xiangchi Liu, Shunlin Tang, Hua Xiang, Guoshun Luo

European Journal of Medicinal Chemistry

DOI

2025

Discovery of a Highly Potent and Selective Tyrosine Kinase 2 (TYK2) Degrader with In Vivo Therapeutic Efficacy in a Murine Psoriasis Model

Shuangshuang Xiong, Jiaqi Yang, Ming Yang, Maoxu Xiao, Si Ha, Wenxiang Tao, Luyu Ma, Chenxuan Ji, Hua Xiang, Guoshun Luo

Journal of Medicinal Chemistry

DOI

2024

Discovery of a highly potent, N-terminal domain-targeting degrader of AR-FL/AR-V7 for the treatment of prostate cancer

Si Ha, Chenxuan Ji, Jiaqi Yang, Maoxu Xiao, Ziyi Xu, Wei-Wei Pan, Hua Xiang, Guoshun Luo

European Journal of Medicinal Chemistry

DOI

2024

Targeting Protein Kinase, Membrane-Associated Tyrosine/Threonine 1 (PKMYT1) for Precision Cancer Therapy: From Discovery to Clinical Trial

Ming Yang, Hua Xiang, Guoshun Luo

Journal of Medicinal Chemistry

DOI

2024

Dual-target inhibitors based on ERα: Novel therapeutic approaches for endocrine resistant breast cancer

Shuangshuang Xiong, Ke Song, Hua Xiang, Guoshun Luo

European Journal of Medicinal Chemistry

DOI

2024

Structure–Activity Relationship (SAR) Studies of Novel Monovalent AR/AR-V7 Dual Degraders with Potent Efficacy against Advanced Prostate Cancer

Maoxu Xiao, Si Ha, Jiacheng Zhu, Wenxiang Tao, Zixuan Fu, Hanlin Wei, Qiangqiang Hou, Guoshun Luo, Hua Xiang

Journal of Medicinal Chemistry

DOI

2024

Discovery and Proof of Concept of Potent Dual Polθ/PARP Inhibitors for Efficient Treatment of Homologous Recombination-Deficient Tumors

Luyu Ma, Wei Chen, Ming Yang, Si Ha, Shuangshuang Xiong, Jiacheng Zhu, Hua Xiang, Guoshun Luo

Journal of Medicinal Chemistry

DOI

2024

Targeting focal adhesion kinase (FAK) for cancer therapy: FAK inhibitors, FAK-based dual-target inhibitors and PROTAC degraders

Ming Jen Yang, Hua Xiang, Guoshun Luo

Biochemical Pharmacology

DOI

2023

X-ray crystallography study and optimization of novel benzothiophene analogs as potent selective estrogen receptor covalent antagonists (SERCAs) with improved potency and safety profiles

Chengfeng Bai, Yang Lv, Shuangshuang Xiong, Shuangjie Wu, Lin Qi, Shengnan Ren, Meiqi Zhu, Haijuan Dong, Hongtao Shen, Zhaoxing Li, Yinxue Zhu, Hui Ye, Haiping Hao, Yibei Xiao, Hua Xiang, Guoshun Luo

Bioorganic Chemistry

DOI

2023

Hydrophobic tag tethering degrader as a promising paradigm of protein degradation: Past, present and future perspectives

Si Ha, Si Ha, Jiacheng Zhu, Jiacheng Zhu, Hua Xiang, Hua Xiang, Guoshun Luo

Chinese Chemical Letters

DOI

2023

Structural optimization of tetrahydroisoquinoline-hydroxamate hybrids as potent dual ERα degraders and HDAC inhibitors

Shuangshuang Xiong, Xin Wang, Meiqi Zhu, Ke Song, Yefan Li, Jiaqi Yang, Xinyan Liu, Mofei Liu, Haijuan Dong, Mingqi Chen, Deying Chen, Hua Xiang, Guoshun Luo

Bioorganic Chemistry

DOI

2022

A Comprehensive Overview of Small-Molecule Androgen Receptor Degraders: Recent Progress and Future Perspectives

Si Ha, Guoshun Luo, Hua Xiang

Journal of Medicinal Chemistry

DOI

2022

Novel 6-amino-1,3,5-triazine derivatives as potent BTK inhibitors: structure-activity relationship (SAR) analysis and preliminary mechanism investigation

Maoxu Xiao, Meiqi Zhu, Shuangjie Wu, Luyu Ma, Lin Qi, Si Ha, Shuangshuang Xiong, Mingqi Chen, Deying Chen, Guoshun Luo, Hua Xiang

Bioorganic Chemistry

DOI

2022

Novel 11β-substituted estradiol conjugates: Transition from ERα agonizts to effective PROTAC degraders

Guoshun Luo, Xinyu Li, Xin Lin, Xiang Lu, Zhenbang Li, Hua Xiang

The Journal of Steroid Biochemistry and Molecular Biology

DOI

2021

“网络课程学习+课堂授课+临床用药案例讨论”三维立体的临床药学专业《药物化学》教学模式研究

徐晓莉，向华，江程

《药学研究》

DOI

2021

Targeting of the FOXM1 Oncoprotein by E3 Ligase-Assisted Degradation

Guoshun Luo, Xin Lin, Antonio Vega-Medina, Maoxu Xiao, Guolong Li, Hanlin Wei, Carlos A. Velázquez‐Martínez, Hua Xiang

Journal of Medicinal Chemistry

DOI

2021

Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer

Guoshun Luo, Xin Lin, Shengnan Ren, Shuangjie Wu, Xin Wang, Luyu Ma, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2021

Design and synthesis of novel benzothiophene analogs as selective estrogen receptor covalent antagonists against breast cancer

Chengfeng Bai, Shengnan Ren, Shuangjie Wu, Meiqi Zhu, Guoshun Luo, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2021

Benzothiophene derivatives as selective estrogen receptor covalent antagonists: Design, synthesis and anti-ERα activities

Chengfeng Bai, Shuangjie Wu, Shengnan Ren, Meiqi Zhu, Guoshun Luo, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2021

Synthesis and evaluation of novel thiosemicarbazone and semicarbazone analogs with both anti-proliferative and anti-metastatic activities against triple negative breast cancer

Chengfeng Bai, Shuangjie Wu, Shengnan Ren, Meiqi Zhu, Guoshun Luo, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2021

Discovery of novel 2H-chromene-3-carbonyl derivatives as selective estrogen receptor degraders (SERDs): Design, synthesis and biological evaluation

Xiang Lu, Yu Teng, Xin Lin, Maoxu Xiao, Chenna Liu, Xinglong Chi, Yulan Zhang, Guoshun Luo, Hua Xiang

Bioorganic Chemistry

DOI

2020

Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity in vivo

Guoshun Luo, Zhenbang Li, Xin Lin, Xinyu Li, Yu Chen, Kun Xi, Maoxu Xiao, Hanlin Wei, Lizhe Zhu, Hua Xiang

Acta Pharmaceutica Sinica B

DOI

2020

Structure-guided modification of isoxazole-type FXR agonists: Identification of a potent and orally bioavailable FXR modulator

Guoshun Luo, Xin Lin, Zhenbang Li, Maoxu Xiao, Xinyu Li, Dayong Zhang, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2020

Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity

Yu Teng, Xinyu Li, Shengnan Ren, Yu Cheng, Kun Xi, Hongtao Shen, Wenzhuo Ma, Guoshun Luo, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2020

Targeting estrogen receptor α for degradation with PROTACs: A promising approach to overcome endocrine resistance

Xin Lin, Hua Xiang, Guoshun Luo

European Journal of Medicinal Chemistry

DOI

2020

Discovery of potent and highly selective covalent inhibitors of Bruton’s tyrosine kinase bearing triazine scaffold

Yu Teng, Xiang Lü, Maoxu Xiao, Zhenbang Li, Yumei Zou, Shengnan Ren, Yu Cheng, Guoshun Luo, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2020

Discovery of novel steroidal-chalcone hybrids with potent and selective activity against triple-negative breast cancer

Qiangqiang Hou, Xin Lin, Xiang Lu, Chengfeng Bai, Hanlin Wei, Guoshun Luo, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2020

A new class of 1,3,5-triazine-based selective estrogen receptor degraders (SERDs): Lead optimization, molecular docking and dynamic simulation

Xiang Lu, Ali Huang, Maoxu Xiao, Liang Sun, Jiashun Mao, Guoshun Luo, Hua Xiang

Bioorganic Chemistry

DOI

2020

Correction: O 2 -3-Aminopropyl diazeniumdiolates suppress the progression of highly metastatic triple-negative breast cancer by inhibition of microvesicle formation via nitric oxide-based epigenetic regulation

Fenghua Kang, Jiayi Zhu, Jianbing Wu, Tian Lv, Hua Xiang, Jide Tian, Yihua Zhang, Zhangjian Huang

Chemical Science

DOI

2019

Design and synthesis of novel steroidal imidazoles as dual inhibitors of AR/CYP17 for the treatment of prostate cancer

Qiangqiang Hou, Conghui He, Kejing Lao, Guoshun Luo, Qidong You, Hua Xiang

Steroids

DOI

2019

Progress in PD-1/PD-L1 pathway inhibitors: From biomacromolecules to small molecules

Xin Lin, Xiang Lu, Guoshun Luo, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2019

Design, synthesis and biological evaluation of novel 2-phenyl pyrimidine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors

Xinyu Li, Binyu Shi, Yu Teng, Yu Cheng, Huizhu Yang, Jiurong Li, Lianjian Wang, Siying He, Qidong You, Hua Xiang

MedChemComm

DOI

2019

Design, synthesis, and biological evaluation of novel androst-17β-amide structurally related compounds as dual 5α-reductase inhibitors and androgen receptor antagonists

Kejing Lao, Guoliang Xun, Xingchun Gou, Hua Xiang

Journal of Enzyme Inhibition and Medicinal Chemistry

DOI

2018

Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ

Linyi Liu, Xinyu Li, Yu Cheng, Lianjian Wang, Huizhu Yang, Jiurong Li, Siying He, Shuangjie Wu, Qianqian Yin, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2018

Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2

Xinyu Li, Cheng-Zhe Wu, Xin Lin, Xuerong Cai, Linyi Liu, Guoshun Luo, Qidong You, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2018

Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity

Guoshun Luo, Zhichao Tang, Kejing Lao, Xinyu Li, Qidong You, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2018

3, 9-di-O-substituted coumestrols incorporating basic amine side chains act as novel apoptosis inducers with improved pharmacological selectivity

Guoshun Luo, Zhengpu Tang, Xinyu Li, Qiangqiang Hou, Yu Chen, Kejing Lao, Hua Xiang

Bioorganic Chemistry

DOI

2018

Structure-guided design and synthesis of isoflavone analogs of GW4064 with potent lipid accumulation inhibitory activities

Rongmao Qiu, Guoshun Luo, Xuerong Cai, Linyi Liu, Mingqi Chen, Deying Chen, Qidong You, Hua Xiang

Bioorganic & Medicinal Chemistry Letters

DOI

2018

Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ

Linyi Liu, Bingyu Shi, Xinyu Li, Xiangqian Wang, Xiang Lu, Xuerong Cai, Ali Huang, Guoshun Luo, Qidong You, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2018

Lipid accumulation inhibitory activities of novel isoxazole-based chenodeoxycholic acids: Design, synthesis and preliminary mechanism study

Rongmao Qiu, Guoshun Luo, Xinyu Li, Fan Zheng, Haolin Li, Jin Zhang, Qidong You, Hua Xiang

Bioorganic & Medicinal Chemistry Letters

DOI

2018

Lipid reducing activity of novel cholic acid (CA) analogs: Design, synthesis and preliminary mechanism study

Guoshun Luo, Zhouyang Qian, Rongmao Qiu, Qidong You, Hua Xiang

Bioorganic Chemistry

DOI

2018

Strategies to Overcome Resistance Mutations of Bruton's Tyrosine Kinase Inhibitor Ibrutinib

Linyi Liu, Bingyu Shi, Xiangqian Wang, Hua Xiang

Future Medicinal Chemistry

DOI

2018

O 2 -3-Aminopropyl diazeniumdiolates suppress the progression of highly metastatic triple-negative breast cancer by inhibition of microvesicle formation via nitric oxide-based epigenetic regulation

Fenghua Kang, Jiayi Zhu, Jianbing Wu, Tian Lv, Hua Xiang, Jide Tian, Yihua Zhang, Zhangjian Huang

Chemical Science

DOI

2017

Novel SERMs based on 3-aryl-4-aryloxy-2H-chromen-2-one skeleton - A possible way to dual ERα/VEGFR-2 ligands for treatment of breast cancer

Guoshun Luo, Xinyu Li, Guoqing Zhang, Cheng-Zhe Wu, Zhengpu Tang, Linyi Liu, Qidong You, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2017

Synthesis and biological evaluation of 4,6-diaryl-2-pyrimidinamine derivatives as anti-breast cancer agents

Linyi Liu, Zhichao Tang, Chengze Wu, Xinyu Li, Ali Huang, Xiang Lu, Qidong You, Hua Xiang

Bioorganic & Medicinal Chemistry Letters

DOI

2017

Design, synthesis and biological evaluation of novel androst-3,5-diene-3-carboxylic acid derivatives as inhibitors of 5α-reductase type 1 and 2

Kejing Lao, Jie Lena Sun, Chong Wang, Weiting Lyu, Boshen Zhou, Ruheng Zhao, Qian Xu, Qidong You, Hua Xiang

Steroids

DOI

2017

Hypolipidemic effect of XH601 on hamsters of Hyperlipidemia and its potential mechanism

Mengjie Zhao, Shanshan Wang, Yao Jiang, Ying Wang, Hong Shen, Pei Xu, Hua Xiang, Hong Xiao

Lipids in Health and Disease

DOI

2017

Design, synthesis and biological evaluation of novel 3-substituted 4-anilino-coumarin derivatives as antitumor agents

Guoshun Luo, Moses Muyaba, Weiting Lyu, Zhichao Tang, Ruheng Zhao, Qian Xu, Qidong You, Hua Xiang

Bioorganic & Medicinal Chemistry Letters

DOI

2016

Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents

Zhichao Tang, Cheng-Zhe Wu, Tianlin Wang, Kejing Lao, Yejun Wang, Linyi Liu, Moses Muyaba, Pei Xu, Conghui He, Guoshun Luo, Zhouyang Qian, Shaoxiong Niu, Lijun Wang, Ying Wang, Hong Xiao, Qidong You, Hua Xiang

European Journal of Medicinal Chemistry

DOI

2016

ChemInform Abstract: Microwave‐Assisted Copper‐ and Palladium‐Catalyzed Sonogashira‐Type Coupling of Aryl Bromides and Iodides with Trimethylsilylacetylene.

Yonghua Lei, Tianhan Hu, Xingsen Wu, Yue Wu, Hua Xiang, Haopeng Sun, Qidong You, Xiaojin Zhang

ChemInform

DOI

2016

Microwave-assisted copper- and palladium-catalyzed sonogashira-type coupling of aryl bromides and iodides with trimethylsilylacetylene

Yonghua Lei, Tianhan Hu, Xingsen Wu, Yue Wu, Hua Xiang, Haopeng Sun, Qidong You, Xiaojin Zhang

Tetrahedron Letters

DOI

2015

Impact of ER520, a candidate of selective estrogen receptor modulators, on in vitro cell growth, migration, invasion, angiogenesis and in vivo tumor xenograft of human breast cancer cells

Lijun Wang, Ying Wang, HUA-QING DU, Yao Xing Jiang, Zhichao Tang, Hongyi Liu, Hua Xiang, Hong Xiao

Cancer Chemotherapy and Pharmacology

DOI

2015

Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton’s tyrosine kinase (BTK) inhibitors

Minhang Xin, Xinge Zhao, Wei Huang, Jin Jun Qiu, Gang Wu, Yazhou Wang, Feng Shii Tang, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2015

An improved and scalable synthesis of N-(5-(4-cyanophenyl)-3-hydroxypicolinoyl)glycine, a promising PHD2 inhibitor for the treatment of anemia

Yonghua Lei, Tianhan Hu, Mingyang Hu, Li Yang, Yue Wu, Hua Xiang, Lianshan Zhang, Lifang Shen, Qidong You, Xiaojin Zhang

Tetrahedron Letters

DOI

2015

Synthesis and biological evaluation of isoflavone amide derivatives with antihyperlipidemic and preadipocyte antiproliferative activities

Wenbin Wang, Yi He, Pei Xu, Qidong You, Hong Xiao, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2015

Pyrrolo[2,3-b]pyridine derivatives as potent Bruton’s tyrosine kinase inhibitors

Xinge Zhao, Wei Huang, Yazhou Wang, Minhang Xin, Jin Jun Qiu, Jianfeng Cai, Feng Shii Tang, Yong Zhao, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2015

Synthesis of Tribolure, the Common Aggregation Pheromone of Four Tribolium Flour Beetles

Chao Wang, Chengyu He, Yong Shi, Hua Xiang, Weisheng Tian

Chinese Journal of Chemistry

DOI

2015

Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton’s tyrosine kinase (BTK) inhibitors

Xinge Zhao, Minhang Xin, Yazhou Wang, Wei Huang, Jin Jun Qiu, Feng Shii Tang, Gang Wu, Yong Zhao, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2014

LC-MS法测定大鼠血浆中EXH-1626的浓度及其药代动力学研究

李泰平，肖红，向华

《实用药物与临床》

2014

Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton’s tyrosine kinase inhibitors

Xinge Zhao, Minhang Xin, Wei Huang, Yanliang Ren, Jin Jun Qiu, Feng Shii Tang, Hai‐Long Jiang, Yazhou Wang, Jie Yang, Shi‐Fu Mo, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2014

Discovery of novel Bruton’s tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold

Xinge Zhao, Wei Huang, Yazhou Wang, Minhang Xin, Jin Jun Qiu, Jianfeng Cai, Feng Shii Tang, Yong Zhao, Hua Xiang

Bioorganic & Medicinal Chemistry

DOI

2014

Discovery of novel aromatase inhibitors using a homogeneous time-resolved fluorescence assay

Jin‐Zi Ji, Kejing Lao, Jie Hu, Tao Pang, Zhenzhou Jiang, Haoliang Yuan, Jingshan Miao, Xin Chen, Shan-shan Ning, Hua Xiang, Yumeng Guo, Ming Yan, Luyong Zhang

Acta Pharmacologica Sinica

DOI

2014

Synthesis and biological evaluation of 2,3-diaryl isoquinolinone derivatives as anti-breast cancer agents targeting ERα and VEGFR-2

Zhichao Tang, Shaoxiong Niu, Fei Liu, Kejing Lao, Jingshan Miao, Jin‐Zi Ji, Xiang Wang, Ming Yan, Luyong Zhang, Qidong You, Hong Xiao, Hua Xiang

Bioorganic & Medicinal Chemistry Letters

DOI

2014

Evaluating the Potential Bioactivity of a Novel Compound ER1626

Lijun Wang, Yanyan Zeng, Tianling Wang, Hongyi Liu, Hong Xiao, Hua Xiang

PLoS ONE

DOI

2013

ChemInform Abstract: New Ligands for Copper‐Catalyzed C—N Coupling Reactions with Aryl Halides.

Dong Chen, Kai Huai Yang, Hua Xiang, Sheng Jiang

ChemInform

DOI

2013

A General and Facile Synthesis of Novel Polysubstituted Quinazolin‐4(3H)‐ones

Minhang Xin, Ying Duo Gao, Hua Xiang, Dong Chen, Yi He, Qidong You

Journal of Heterocyclic Chemistry

DOI

2012

新型6-芳基茚并异喹啉酮衍生物的合成及抗肿瘤活性研究

王天麟，向华，徐晓莉，肖红，尤启冬

《中国药物化学杂志》

2012

New ligands for copper-catalyzed C–N coupling reactions with aryl halides

Dong Chen, Kai Huai Yang, Hua Xiang, Sheng Jiang

Tetrahedron Letters

DOI

2011

2甲-氧基雌二醇-RGD肽缀合物的合成及其抗血管生成作用(英文)

辛敏行，向华，司文博，赵维，肖红，尤启冬

《中国药科大学学报》

2011

A Review on Steroidal 5α-Reductase Inhibitors for Treatment of Benign Prostatic Hyperplasia

Jingyuan Sun, Hua Xiang, Lin Yang, J.-B. Chen

Current Medicinal Chemistry

DOI

2011

Synthesis and biological evaluation of new flavonoid fatty acid esters with anti-adipogenic and enhancing glucose consumption activities

Wei Zhao, Jie Lena Sun, Hua Xiang, Yanyan Zeng, Xiaobo Li, Hong Xiao, Deying Chen, Ren-ling Ma

Bioorganic & Medicinal Chemistry

DOI

2010

Synthesis and biological evaluation of isoflavone fatty acid esters with potential weight loss and hypolipidemic activities

Hua Xiang, Wei Zhao, Hong Xiao, Lei Qian, Yao Yao, Xiaobo Li, Liao Qing-jiang

Bioorganic & Medicinal Chemistry

DOI

2009

An efficient, practical synthesis of 2-methoxyestradiol

Minhang Xin, Qidong You, Hua Xiang

Steroids

DOI

2007

减肥药物最新研究进展

钱磊，向华，尤启冬，廖清江

《中国新药杂志》

2006

治疗乳腺癌的抗雌激素药物研究进展

冯长根，邓霞飞，向华，廖清江

《中国新药杂志》

2006

大豆黄素衍生物的合成及其与雌激素受体亲和力的研究

向华，方维，何玲，张陆勇，廖清江

《中国药科大学学报》

2006

2-芳亚胺基-4-噻唑烷酮类化合物的合成及生物活性

张大永，向华，徐云根，华维一

《药学学报》

2005

骨生长肽的研究进展

冯长根，邓霞飞，杨艳青，向华

《中国药学杂志》

2004

Enzymatic synthesis of a CCK‐8 tripeptide fragment

Hua Xiang, Heiner Eckstein

Chinese Journal of Chemistry

DOI

2004

Total enzymatic synthesis of cholecystokinin CCK-5

Hua Xiang, Guangya Xiang, Zimin Lü, Li Guo, Heiner Eckstein

Amino Acids

DOI

2003

6-甲氧基-2-(4-甲氧苯基)苯并[b]噻吩及其异构体的合成研究

向华，廖清江

《中国药物化学杂志》

2001

选择性雌激素受体调节剂有关药物的研究进展

向华，廖清江

《中国药房》

精选作品

期刊论文

Optimization of a Second-Generation, Highly Selective Polθ/PARP1 Dual Inhibitor with Improved Pharmacokinetics and Potent Activity against HR-Deficient Tumors

Discovery of an orally bioavailable selenium-containing Polθ inhibitor with a dual mechanism of DNA damage and immune activation for HR-deficient cancers

Approved Steroidal Drugs (2000–2025): A Medicinal Chemistry Perspective

The PROTAC milestone: FDA approval of vepdegestrant (ARV-471) for ESR1-mutated breast cancer

A patent review of DNA polymerase theta (Polθ) targeted therapies (2019–2025)

Lysine-targeted covalent inhibitors: mechanistic advances, pharmacological perspectives and translational challenges

Targeted degradation of Werner syndrome helicase (WRN) via ligand-directed covalent hydrophobic tagging

Discovery of a Highly Potent and Selective Tyrosine Kinase 2 (TYK2) Degrader with In Vivo Therapeutic Efficacy in a Murine Psoriasis Model

Discovery of a highly potent, N-terminal domain-targeting degrader of AR-FL/AR-V7 for the treatment of prostate cancer

Targeting Protein Kinase, Membrane-Associated Tyrosine/Threonine 1 (PKMYT1) for Precision Cancer Therapy: From Discovery to Clinical Trial

Dual-target inhibitors based on ERα: Novel therapeutic approaches for endocrine resistant breast cancer

Structure–Activity Relationship (SAR) Studies of Novel Monovalent AR/AR-V7 Dual Degraders with Potent Efficacy against Advanced Prostate Cancer

Discovery and Proof of Concept of Potent Dual Polθ/PARP Inhibitors for Efficient Treatment of Homologous Recombination-Deficient Tumors

Targeting focal adhesion kinase (FAK) for cancer therapy: FAK inhibitors, FAK-based dual-target inhibitors and PROTAC degraders

X-ray crystallography study and optimization of novel benzothiophene analogs as potent selective estrogen receptor covalent antagonists (SERCAs) with improved potency and safety profiles

Hydrophobic tag tethering degrader as a promising paradigm of protein degradation: Past, present and future perspectives

Structural optimization of tetrahydroisoquinoline-hydroxamate hybrids as potent dual ERα degraders and HDAC inhibitors

A Comprehensive Overview of Small-Molecule Androgen Receptor Degraders: Recent Progress and Future Perspectives

Novel 6-amino-1,3,5-triazine derivatives as potent BTK inhibitors: structure-activity relationship (SAR) analysis and preliminary mechanism investigation

Novel 11β-substituted estradiol conjugates: Transition from ERα agonizts to effective PROTAC degraders

“网络课程学习+课堂授课+临床用药案例讨论”三维立体的临床药学专业《药物化学》教学模式研究

Targeting of the FOXM1 Oncoprotein by E3 Ligase-Assisted Degradation

Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer

Design and synthesis of novel benzothiophene analogs as selective estrogen receptor covalent antagonists against breast cancer

Benzothiophene derivatives as selective estrogen receptor covalent antagonists: Design, synthesis and anti-ERα activities

Synthesis and evaluation of novel thiosemicarbazone and semicarbazone analogs with both anti-proliferative and anti-metastatic activities against triple negative breast cancer

Discovery of novel 2H-chromene-3-carbonyl derivatives as selective estrogen receptor degraders (SERDs): Design, synthesis and biological evaluation

Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity in vivo

Structure-guided modification of isoxazole-type FXR agonists: Identification of a potent and orally bioavailable FXR modulator

Discovery of novel quinazoline derivatives as potent PI3Kδ inhibitors with high selectivity

Targeting estrogen receptor α for degradation with PROTACs: A promising approach to overcome endocrine resistance

Discovery of potent and highly selective covalent inhibitors of Bruton’s tyrosine kinase bearing triazine scaffold

Discovery of novel steroidal-chalcone hybrids with potent and selective activity against triple-negative breast cancer

A new class of 1,3,5-triazine-based selective estrogen receptor degraders (SERDs): Lead optimization, molecular docking and dynamic simulation

Correction: O 2 -3-Aminopropyl diazeniumdiolates suppress the progression of highly metastatic triple-negative breast cancer by inhibition of microvesicle formation via nitric oxide-based epigenetic regulation

Design and synthesis of novel steroidal imidazoles as dual inhibitors of AR/CYP17 for the treatment of prostate cancer

Progress in PD-1/PD-L1 pathway inhibitors: From biomacromolecules to small molecules

Design, synthesis and biological evaluation of novel 2-phenyl pyrimidine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors

Design, synthesis, and biological evaluation of novel androst-17β-amide structurally related compounds as dual 5α-reductase inhibitors and androgen receptor antagonists

Optimization of novel benzofuro[3,2-b]pyridin-2(1H)-one derivatives as dual inhibitors of BTK and PI3Kδ

Synthesis and biological evaluation of 3-aryl-quinolin derivatives as anti-breast cancer agents targeting ERα and VEGFR-2

Structure-activity relationships of 2, 4-disubstituted pyrimidines as dual ERα/VEGFR-2 ligands with anti-breast cancer activity

3, 9-di-O-substituted coumestrols incorporating basic amine side chains act as novel apoptosis inducers with improved pharmacological selectivity

Structure-guided design and synthesis of isoflavone analogs of GW4064 with potent lipid accumulation inhibitory activities

Design and synthesis of benzofuro[3,2-b]pyridin-2(1H)-one derivatives as anti-leukemia agents by inhibiting Btk and PI3Kδ

Lipid accumulation inhibitory activities of novel isoxazole-based chenodeoxycholic acids: Design, synthesis and preliminary mechanism study

Lipid reducing activity of novel cholic acid (CA) analogs: Design, synthesis and preliminary mechanism study

Strategies to Overcome Resistance Mutations of Bruton's Tyrosine Kinase Inhibitor Ibrutinib

O 2 -3-Aminopropyl diazeniumdiolates suppress the progression of highly metastatic triple-negative breast cancer by inhibition of microvesicle formation via nitric oxide-based epigenetic regulation

Novel SERMs based on 3-aryl-4-aryloxy-2H-chromen-2-one skeleton - A possible way to dual ERα/VEGFR-2 ligands for treatment of breast cancer

Synthesis and biological evaluation of 4,6-diaryl-2-pyrimidinamine derivatives as anti-breast cancer agents

Design, synthesis and biological evaluation of novel androst-3,5-diene-3-carboxylic acid derivatives as inhibitors of 5α-reductase type 1 and 2

Hypolipidemic effect of XH601 on hamsters of Hyperlipidemia and its potential mechanism

Design, synthesis and biological evaluation of novel 3-substituted 4-anilino-coumarin derivatives as antitumor agents

Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti-breast cancer agents

ChemInform Abstract: Microwave‐Assisted Copper‐ and Palladium‐Catalyzed Sonogashira‐Type Coupling of Aryl Bromides and Iodides with Trimethylsilylacetylene.

Microwave-assisted copper- and palladium-catalyzed sonogashira-type coupling of aryl bromides and iodides with trimethylsilylacetylene

Impact of ER520, a candidate of selective estrogen receptor modulators, on in vitro cell growth, migration, invasion, angiogenesis and in vivo tumor xenograft of human breast cancer cells

Synthesis and biological evaluation of novel 7-substituted 3-(4-phenoxyphenyl)thieno[3,2-c]pyridin-4-amines as potent Bruton’s tyrosine kinase (BTK) inhibitors

An improved and scalable synthesis of N-(5-(4-cyanophenyl)-3-hydroxypicolinoyl)glycine, a promising PHD2 inhibitor for the treatment of anemia

Synthesis and biological evaluation of isoflavone amide derivatives with antihyperlipidemic and preadipocyte antiproliferative activities

Pyrrolo[2,3-b]pyridine derivatives as potent Bruton’s tyrosine kinase inhibitors

Synthesis of Tribolure, the Common Aggregation Pheromone of Four Tribolium Flour Beetles

Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton’s tyrosine kinase (BTK) inhibitors

LC-MS法测定大鼠血浆中EXH-1626的浓度及其药代动力学研究

Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton’s tyrosine kinase inhibitors

Discovery of novel Bruton’s tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold

Discovery of novel aromatase inhibitors using a homogeneous time-resolved fluorescence assay

Synthesis and biological evaluation of 2,3-diaryl isoquinolinone derivatives as anti-breast cancer agents targeting ERα and VEGFR-2

Evaluating the Potential Bioactivity of a Novel Compound ER1626

ChemInform Abstract: New Ligands for Copper‐Catalyzed C—N Coupling Reactions with Aryl Halides.

A General and Facile Synthesis of Novel Polysubstituted Quinazolin‐4(3H)‐ones

新型6-芳基茚并异喹啉酮衍生物的合成及抗肿瘤活性研究

New ligands for copper-catalyzed C–N coupling reactions with aryl halides

2甲-氧基雌二醇-RGD肽缀合物的合成及其抗血管生成作用(英文)

A Review on Steroidal 5α-Reductase Inhibitors for Treatment of Benign Prostatic Hyperplasia

Synthesis and biological evaluation of new flavonoid fatty acid esters with anti-adipogenic and enhancing glucose consumption activities

Synthesis and biological evaluation of isoflavone fatty acid esters with potential weight loss and hypolipidemic activities