XIANG,HUA

1. Anticancer drug discovery targeting steroid hormone receptors or enzymes.

2. Drugs for senile diseases (menopausal osteoporosis, menopausal syndrome, benign prostatic hyperplasia, hyperlipidaemia, Alzheimer's disease, etc.).

3. Steroidal drugs:  R&D, synthesis improvement with suitable natural steroidal sapogenins as starting materials.

Education

Work Experience

Research Projects

1. Design, bioactivity and mechanism of anti-breast cancer drugs based on the dual targets of ERα and VEGFR-2 (Project supported by the National Natural Science Foundation, No. 81373279), 2014-2017

2. Research and Development of a Novel Lipid Regulator Candidate. (Project supported by the Twelfth Five-Year Plan Major Project of Candidate Drugs, Ministry of National Science and Technology, No. 2012ZX09103101041), 2012-2015

3. Nanjing “321” Technological Entrepreneurial Leading Talent Project：Novel Drug and Active Pharmaceutical Intermediates  R & D and Industrialization, 2013-2016

4.  Jiangsu Province “Six Talent Peaks” Project: Design, Synthesis of Lipid Regulators Targeting CETP. 2014-2016

5. Research and Development of a Novel Anti-breast Cancer (ER+) Drug Candidate. (Project supported by the Twelfth Five-Year Plan Major Project of Candidate Drugs, Ministry of National Science and Technology, No. 2012ZX09103101048), 2012-2015

6. Drug synthesis and New Drug discovery targeting steroid hormone receptors (project supported by the Scientific Development Program of Jiangsu Province, No. BE2012745 and No. BZ2008058), 2013-2015, 2009-2011

7. Synthesis of Adrenocorticoid Drugs from Hecogenin. National Project of Demonstration for High-tech Industrialization, 2008-2012

8. R&D and Approval of Finasteride, Sibutramine, etc in China for ZhengQing Pharm (Approval No. H20050328, H20050329, H20030654), 1999-2005

9. R&D and Approval of a series of agents of Sinomenine Hydrochloride (tablets, sustained tablets, injection, drops) for ZhengQing Pharm, 1996-2002

Lecturing

Publications

1. Zhichao Tang, Chengzhe Wu, Tianlin Wang, Kejing Lao, Yejun Wang, Linyi Liu, Shaoxiong Niua, Lijun Wang, Ying Wang, Qidong Youa, Hong Xiao, Hua Xiang*. Design, synthesis and evaluation of 6-aryl-indenoisoquinolone derivatives dual targeting ERα and VEGFR-2 as anti- breast cancer agents. European Journal of Medicinal Chemistry 2016, 118, 328-339.

2. Minhang Xin*, Xinge Zhao, Wei Huang, Qiu Jin, Gang Wu, Yazhou Wang, Feng Tang, Hua Xiang*. 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. Bioorganic & Medicinal Chemistry, 2015, 23(19): 6250-6257.

3. Shaoxiong Niu, Zhichao Tang, Chang Liu, Tianlin Wang, Qidong You, Hua Xiang*. An Improved Synthesis of 6-Arylindenoisoquinoline Derivatives. Organnic Chemistry (in Chinese). 2015, 35, 2150-2156 .

4. Xinge Zhao, Minhang Xin, Yazhou Wang, Wei Huang, Qiu Jin, Feng Tang, Gang Wu, Yong Zhao, Hua Xiang*. Discovery of thieno [3,2-c]pyridin-4-amines as novel Bruton’s tyrosine kinase (BTK) inhibitors. Bioorganic & Medicinal Chemistry, 2015, 23(17): 6059-6068.

5. Wenbin Wang, Yi He, Pei Xu, Qidong You, Hong Xiao, Hua Xiang*. Synthesis and biological evaluation of isoflavone amide derivatives with antihyperlipidemic and preadipocyte antiproliferative activities. Bioorganic & Medicinal Chemistry, 2015, 23 (15): 4428-4433.

6. Xinge Zhao, Wei Huang, Yazhou Wang, Minhang Xin, Qiu Jin, Jianfeng Cai, Feng Tang, Yong Zhao, Hua Xiang*. Pyrrolo [2,3-b]pyridine derivatives as potent Bruton’s tyrosine kinase inhibitors. Bioorganic & Medicinal Chemistry, 2015, 23(15): 4344-4353.

7. Xinge Zhao, Wei Huang, Yazhou Wang, Minhang Xin, Qiu Jin, Jianfeng Cai, Feng Tang, Yong Zhao, Hua Xiang*. Discovery of novel Bruton’s tyrosine kinase (BTK) inhibitors bearing a pyrrolo [2,3-d]pyrimidine scaffold. Bioorganic & Medicinal Chemistry, 2015, 23(4): 891-901.

8. Xinge Zhao, Minhang Xin, Wei Huang, Yanliang Ren, Qiu Jin, Feng Tang, Hailong Jiang, Yazhou Wang, Jie Yang, Shifu Mo, Hua Xiang*. Design, synthesis and evaluation of novel 5-phenylpyridin-2(1H)-one derivatives as potent reversible Bruton’s tyrosine kinase inhibitors. Bioorganic & Medicinal Chemistry, 2015, 23(2): 348-364.

9. Tang ZC, Niu SX, Liu F, Lao KJ, Miao JS, Ji JZ, Wang X, Yan M, Zhang LY, You QD, Xiao H, Xiang H*. Synthesis and biological evaluation of 2, 3-diaryl isoquinolinone derivatives as anti-breast cancer agents targeting ERα and VEGFR-2. Bioorg Med Chem Lett. 2014, 24(9): 2129-33

10. Wang L, Zeng Y, Wang T, Liu H, Xiao H, Xiang H*. Evaluating the potential bioactivity of a novel compound ER1626. PLoS One. 2014, 9(1): 1-9

11. Minhang Xin, Ying Gao, Hua Xiang*, Dong Chen, Yi He, Qidong You. A general and facile synthesis of novel polysubstituted quinazolin-4(3H)-ones. Journal of Heterocyclic Chemistry, 2013, 50(1): 169-174.

12. Chen D, Yang K, Xiang H*, Jiang S. New ligands for copper-catalyzed C–N coupling reactions with aryl halides. Tetrahedron Lett, 2012; 53:7121-7124..

13. Jie Sun, Hua Xiang*, Lila Yang, Jiabao Chen. A Review on Steroidal 5α-Reductase Inhibitors for Treatment of Benign Prostatic Hyperplasia. Current Medicinal Chemistry, 2011, 18 (23): 3576-3589 .

14. Wei Zhao, Jie Sun, Hua Xiang*, Yanyan Zeng, Xiaobo Li, Hong Xiao, Deying Chen Renling Ma. Synthesis and biological evaluation of new Flavonoid Fatty Acid Esters with anti-adipogenic and enhancing glucose consumption activities. Bioorganic & Medicinal Chemistry. 2011, 19: 3192–3203 .

15. Jie Jiao, Hua Xiang*, Qingjiang Liao. Recent advancement in nonsteroidal aromatase inhibitors for treatment of estrogen-dependent breast cancer. Current Medicinal Chemistry, 2010, 17 (30): 3476-3487 .

16. Hua Xiang*, Wei Zhao, Hong Xiao, et al. Synthesis and biological evaluation of Isoflavone Fatty Acid Esters with potential weight loss and hypolipidemic activities. Bioorganic & Medicinal Chemistry, 2010, 18: 3036–3042 .

17. Minhang Xin, Qidong You, Hua Xiang*. An efficient, practical synthesis of 2-methoxyestradiol. Steroids, 2010, 75 (1) : 53–56 .

18. Tianlin Wang, Qidong You, Hua Xiang*. Recent Advances in Selective Estrogen Receptor Modulators for Breast Cancer. Mini-review in medicinal chemistry, 2009, 9, 1191-1201.

19. Ling He, Hua Xiang, Lu-Yong Zhang, etc. Novel Estrogen Receptor Ligands and Their Structure-Activity Relationship Evaluated by Scintillation Proximity Assay for High-Throughput Screening. Drug Development Research, 2005, 51:1-10 .

20. Hua Xiang, Guang-Ya Xiang, H. Eckstein*. Enzymatic Synthesis of a CCK-8(4-6) Tripeptide Fragment. Chinese Journal of Chemistry, 2004, 22: 1138-1141.

21. Hua. Xiang, G. Xiang, H. Eckstein*, Total enzymatic synthesis of cholecystokinin CCK-5, Amino Acids, 2004, 27: 101-105.

Patents

1. Hua Xiang, Lei Qian, Wei Zhao, et al. Isoflavone Fatty Acid Ester Derivatives, Preparation Methods and Medicinal Uses Thereof. ZL 2008 1 0156213.8

2. Hua Xiang, Yu Zeng, Huifen Liang, et al. Synthesis Improvement of Finasteride. ZL2001 1 01935.2，2001

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