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向华,博士,药学院药物化学教授,博士生导师。
学习和工作经历:
1985.7四川大学化学系有机化学专业学士;
1988.7四川大学化学系有机分析专业硕士;
1988.7-2000.9湖南省中医药研究院新药研发省级重点实验室、湖南正清制药集团新药研发中心从事药物化学和新药研发工作;
2003.12中国药科大学药学院药物化学专业博士;
2002.8-2003.9 Institute of Organic Chemistry,University of Tuebingen,Germany(德国蒂宾根大学博士联合培养)
2014.9-2015.9 Koch Institute for Integrative Cancer Research,Massachusetts Institute of Technology,USA(美国麻省理工学院访问学者)
研究方向:
主要从事抗肿瘤和抗代谢性疾病药物研究,重点开展与性激素代谢紊乱有关的肿瘤(乳腺癌、子宫内膜癌、卵巢癌、前列腺癌等)和老年病(更年期骨质疏松、良性前列腺增生、血脂异常、II型糖尿病等)治疗药物的研究与开发;此外,还从事甾体新药开发及老品种合成工艺改进、甾体新资源的开发和利用。
承担科研项目:
1.主持国家自然科学基金面上项目(ER/VEGFR双靶点抗乳腺癌药物研究,81373279);
2.主持科技部“重大新药创制”科技重大专项(调血脂候选药研究,2012ZX09103101-041);
3.主持江苏省科技支撑计划-社会发展项目(抗乳腺癌药物研究,BE2012745);
4.主持江苏省“六大人才高峰”项目(基于CETP的调血脂药物分子发现及活性研究,2013-YY003);
5.主持南京市321领军型科技创业人才计划项目:创新药物及医药中间体研发及产业化;
6.主持江苏省国际合作项目(SERM化合物设计、合成及生物活性,BZ2008058);
7.主持国家发改委西部高技术产业化示范工程子项:蕃蔴二烯物合成甾体激素药物的研究;
8.参加科技部“重大新药创制”科技重大专项(抗乳腺癌候选药物,2012ZX09103101-048);
9.参加国家自然基金重点项目(具有NRF2-Keap1蛋白-蛋白相互调控作用的类天然产物研究,81230078)。
10.与多家甾体激素制药企业合作,主持多项新药研究项目,作为项目负责人获得新药证书三本,负责开发的多个原料药品种投放生产。
承担教学:
主讲课程:高等有机化学(研究生课程)、药物化学(本科生课程)等;
指导博士及硕士研究生学位论文、本科生毕业实践、创新实践项目、开放性实验项目等。
近期论文:
1.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
2.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
3.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
4.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
5.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
6.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): 2129-2133
7.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
8.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
9.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
10.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
11.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
12.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
13..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
14..Minhang Xin, Qidong You, Hua Xiang*. An efficient, practical synthesis of 2-methoxyestradiol. Steroids, 2010, 75 (1) : 53-56
15..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
近期专利:
1.Hua Xiang, Tianlin Wang, Hong Xiao, Qidong You,Yao Yao, Xiaobo Li, Qingjiang Liao. Inden[1, 2-b]isoquinolinone derivatives, production and use thereof as a medicament. US8664238 B2. WO 2011047515 A1.(授权)
2.Hua Xiang, Wei Zhao, Hong Xiao, Yao Yao, Renling Ma, Lei Qian, Xiaobo Li, Qidong You, Qingjiang Liao. Isoflavone Fatty Acid Ester Derivatives, Preparation Methods and Medicinal Uses Thereof. US8846752 B2, WO2011106924 A1.(授权)
3.向华,劳可静,唐智超,严明,宁珊珊,张陆勇,尤启冬.4-咪唑基喹啉酮类芳香化酶抑制剂、制备方法和医药用途.ZL201310081971.9(授权)
4.向华,宁珊珊,刘元元,孙洁,寻国良,严明,徐旭东,张陆勇,廖清江,尤启冬.甾体类5α-还原酶抑制剂、其制备方法及其医药用途.ZL201210001077.1(授权)
5.向华,王文宾,肖红等.异黄酮酰胺类衍生物、其制备方法和医药用途.CN201510106301.7
6.向华,牛绍雄,唐智超等;trans-四氢异喹啉酮-4-羧酸衍生物的合成方法与医药用途.CN201510180778.X
7.向华,唐郑普,骆国顺等.香豆雌酚开环类似物及其医药用途:中国专利,201510113977.9
8.向华,劳可静,何聪慧,唐郑普,严明,肖红,尤启冬.甾体类雄激素受体抑制剂、其制备方法及其医药用途.2014,CN103694299A.
9.向华,刘元元,辛敏行,司文博,林森森,张陆勇.一类作为血管抑制剂的雌甾衍生物、其制备方法和医药用途.2013,CN102952168A.
10.向华,何怡,赵维,肖红.异黄酮或类黄酮脂肪醚类衍生物、其制备方法和医药用途,CN102964322A
11.向华,司文博,刘元元,严明,肖红,尤启冬,张陆勇,廖清江.喹唑啉酮类血管抑制剂、其制备方法及其医药用途.CN102875480A.
12.向华,宁珊珊,刘元元,孙洁,寻国良,严明,徐旭东,张陆勇,廖清江,尤启冬.甾体类5α-还原酶抑制剂、其制备方法及其医药用途.CN102532236A
13..向华,赵维,辛敏行,李骁博,陈德英,马仁玲,廖清江.类黄酮脂肪酸酯类衍生物、其制备方法和医药用途.CN102603685A
14..向华,王天麟,肖红,尤启冬,姚瑶,李骁博,廖清江.茚并异喹啉酮衍生物、其制备方法及其医药用途.ZL200910233991.7(授权)
15.向华,钱磊,赵维,巫冠中,廖清江.大豆黄素脂肪酸酯类衍生物、其制备方法和医药用途.ZL200810156213.8(授权)
联络方式:
Tel:025-83271096(Tel/Fax);E-mail:cpuxianghua@163.com
通信地址:南京市童家巷24号,中国药科大学药学院药物化学教研室,邮编210009
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