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中国科学院上海药物研究所导师教师师资介绍简介-杨春皓

本站小编 Free考研考试/2021-02-10

xm:杨春皓
xb:男
zc:研究员
xl:博士
dh:+86-
cz:
dzyj:chyang@simm.ac.cn
grzy:
zjlb:研究员;新药;
zw:研究组长,博士生导师
txdz:上海市浦东新区祖冲之路555号
grjj: 杨春皓现为上海药物研究所研究员、博士生导师、课题组长。作为课题负责人目前承担着多项国家项目,包括“十三五”重大专项子课题、国家自然基金及中国科学院战略先导科技专项A子课题等,共发表同行评审文章九十多篇,申请国内国际专利二十多项,2017年入选中国科学院“特聘骨干人才”。


yjfx:新型抗肿瘤药物、骨相关疾病药物的研发;生物活性为导向的杂环方法学研究
dblz:近五年代表性论著

1. Hao-Yue Xiang , Yan-Hong Chen, Yi Wang, Xi Zhang, Jian Ding, Ling-Hua Meng* and Chun-Hao Yang*. Design, synthesis and antiproliferative activity evaluation of a series of pyrrolo[2,1-f][1,2,4]triazine derivatives. Bioorg. Med. Chem. Lett. 2020, DOI : 10.1016/j.bmcl.2020.127194

2. Fangran Liu, Xiaofei Zhang, Qun Qian *, Chunhao Yang*. A Concise and Efficient Approach to 2,6-disubstituted-4-Fluoro-pyrimidines from α-CF3 Aryl Ketones. Synthesis. 2020; 52(02): 273-280.

3. Yingyuan Peng, Qian He, Xiaofei Zhang* and Chunhao Yang*. Pd-catalyzed Intramolecular C–H Activation and C–S Formation to Synthesize Pyrazolo[5, 1-b]benzothiazoles without an Additional Oxidant. Org. Chem. Front. 2019, 6, 3234-3237.

4.Min Jiang, Lei Peng, Kai Yang, Tianqi Wang, Xueming Yan, Tao Jiang, Jianrong Xu, Jin Qi, Hanbing Zhou, Niandong Qian, Qi Zhou, Bo Chen, Xing Xu*, Lianfu Deng*, Chunhao Yang* Development of Small Molecules Targeting Receptor Activator of Nuclear Factor-κB Ligand (RANKL) - Receptor Activator of Nuclear Factor-κB (RANK) Protein-Protein Interaction by Structure-Based Virtual Screening and Hit Optimization. J. Med. Chem., 2019, 62, 5370-5381.

5. Tianzi Dai Qunyi Li, Xiaofei Zhang*, and Chunhao Yang.* Substituent-Oriented Synthesis of Substituted Pyrazoles/ Chromeno[3,2-c]Pyrazoles via Sequential Reactions of Chromones/3-chlorochromones and Tosylhydrazones. J. Org. Chem. 2019, 84 (9), 5913–5921.

6. Xiaofeng Peng, Xiaofei Zhang, Shunyao Li, Yunfu Lu, Lefu Lan * and Chunhao Yang.* Silver-mediated Synthesis of Novel 3-CF3/CN/Phosphonate-substituted Pyrazoles as Pyrrolomycin Analogues from 3-Formylchromones and Diazo Compounds. Org. Chem. Front. 2019, 6, 1775 – 1779.

7. Min Jiang , Tianqi Wang, Xueming Yan, Zhuochao Liu, Yufei Yan, Kai Yang, Jin Qi, Hanbing Zhou, Niandong Qian, Qi Zhou, Bo Chen, Xing Xu*, Xiaobing Xi*, Chunhao Yang*, Lianfu Deng. A novel rhein derivative modulates bone formation and resorption and ameliorates oestrogen-dependent bone loss. J. Bone Miner. Res. 2019, 34(2), 361-374.

8. Bo Jiang, Xiaofei Zhang and Chunhao Yang*. Palladium-catalyzed direct approach to α-CF3 aryl ketones from arylboronic acids. Org. Chem. Front., 2018, 5, 1724-1727.

9. Xuxing Chen, Xiajuan Huan, Qiufeng Liu,YuqinWang, Qian He, Cun Tan, Yi Chen, Jian Ding, Yechun Xu,* Zehong Miao,* and Chunhao Yang*. Design and Synthesis of 2-(4,5,6,7-Tetrahydrothienopyridin-2-yl)-benzoimidazole Carboxamides as Novel Orally Efficacious Poly(ADP-ribose)polymerase (PARP) Inhibitors. Eur. J. Med. Chem. 2018, 145, 389-403.

10. Jing Li, Xiaofei Zhang, Haoyue Xiang, Linjiang Tong, Fang Feng, Hua Xie, Jian Ding, and Chunhao Yang.* C-H Trifluoromethylation of 2-Substitued/Unsubstituted-amino-naphthoquinones at Room Temperature with Bench-stable (CF3SO2)2Zn: Synthesis and Antiproliferative Evaluation. J. Org. Chem. 2017, 82, 6795-6800.

11. Bin Zhang, Xiaofei Zhang, Jian Hao,* and Chunhao Yang.* Direct Approach to N-Substituted-2-Fluoroindoles by Sequential Construction of C-N Bonds from gem-Difluorostyrenes. Org. Lett., 2017, 19 (7), 1780–1783.

12. Jin-Xue He, Meng Wang, Xia-Juan Huan, Chuan-Huizi Chen, Shan-Shan Song, Ying-Qing Wang, Xue-Mei Liao, Cun Tan, Qian He, Lin-Jiang Tong, Yu-Ting Wang, Xiao-Hua Li, Yi Su, Yan-Yan Shen, Yi-Ming Sun, Xin-Ying Yang, Yi Chen, Zhi-Wei Gao, Xiao-Yan Chen, Bing Xiong, Xiu-Lian Lu, Jian Ding, Chun-Hao Yang,* Ze-Hong Miao.* Novel PARP1/2 inhibitor mefuparib hydrochloride elicits potent in vitro and in vivo anticancer activity, characteristic of high tissue distribution. Oncotarget. 2017 ;8(3):4156-4168.

13. Xing Xu, Xueyu Qi, Yufei Yan, Jin Qi, Niandong Qian, Lei Guo, Changwei Li, Fei Wang, Ping Huang, Hanbing Zhou, Min Jiang, * Chunhao Yang* and Lianfu Deng. Synthesis and biological evaluation of rhein amides as inhibitors of osteoclast differentiation and bone resorption. Eur. J. Med. Chem. 2016, 123, 769-776.

14. Xia Liu, Zhijian Xu, Chuanwei Hou, Meng Wang, Xinhuan Chen, Qinghui Lin, Rui Song, Meng Lou, Lijun Zhu, Yunqing Qiu, Zhi Chen, Chunhao Yang*, Weiliang Zhu*, Jimin Shao.* Inhibition of hepatitis B virus replication by targeting ribonucleotide reductase M2 protein. Biochemical Pharmacology, 2016, 103, 118-128.

15. Xueyu Qi, Haoyue Xiang, and Chunhao Yang * Synthesis of functionalized chromeno[2,3-b]pyrrol-4(1H)-ones by silver-catalyzed cascade reactions of chromones/thiochromones and isocyanoacetates. Org. Lett. 2015, 17, 5590-5593.

16. Min Jiang, Haoyue Xiang, Fangxia Zhu, Xing Xu, Lianfu Deng, * and Chunhao Yang.* Efficient Pd-catalyzed domino synthesis of 1-phenyl-1H-indol-2-amine and 5-amino-indolo[1,2-a]quinazoline derivatives. Org. Biomol. Chem., 2015, 13, 10122-10126. (Highlighted by Synfacts, 2015, 11(12), 1250)

17. Xiaofei Zhang, and Chunhao Yang* Alkylations of Aryl Boronic Acids including Difluoroethylation/Trifluoroethylation via Nickel-Catalyzed Suzuki Cross-Coupling Reaction. Adv. Synth. Catal. 2015, 357, 2721-2727.

18. Min Jiang, Fangxia Zhu, Haoyue Xiang, Xing Xu, Lianfu Deng,* and Chunhao Yang.* An Efficient and Practical Approach to Trifluoromethylthiolation of α-Haloketones/α-Haloarylmethanes. Org. Biomol. Chem., 2015, 13, 6935 – 6939.

19. Jun-Mei Yi,Xiao-Fei Zhang,Xia-Juan Huan,Shan-Shan Song, Wei Wang, Qian-Ting Tian, Yi-Ming Sun, Yi Chen, Jian Ding, Ying-Qing Wang,* Chun-Hao Yang,* Ze-Hong Miao.* Dual Targeting of Microtubule and Topoisomerase II by α-Carboline Derivative YCH337 for Tumor Proliferation and Growth Inhibition. Oncotarget, 2015, 6,11, 8960-8973.


jyjl:苏州大学化学系,本科
华东师范大学化学系,硕士中国科学院上海药物研究所,博士佐治亚州立大学化学系,访问****
gzjl:南通医学院,讲师佐治亚州立大学化学系,访问****上海药物研究所,助研、副研、研究员
ktxm:国家自然基金委,ERRα反向激动剂的优化设计及抗肿瘤活性和机制研究,项目负责人中国科学院战略先导科技专项(A类),易透过血脑屏障的抗肿瘤候选新药盐酸美呋哌瑞的临床个性化研究,子课题负责人“十三五”新药创制重大专项,PARP抑制剂盐酸美呋哌瑞的临床研究,课题负责人
ryhj:上海市科技进步三等奖明治生命科学奖中国科学院朱李月华优秀教师奖
xpwj:http://sourcedb.simm.cas.cn/zw/gb2020/yjzz/202008/P.jpg
kycg: 1.本课组在杂环化合物库的构建、高品质苗子/先导化合物的发现方面取得了一定进展。建立了基于化学反应的结构多样性化合物库、基于抗肿瘤热点靶标的集中化合物库、基于活性的类天然化合物库等,从中发现了多个高活性化合物,在此基础上发现了一些机制新颖的抗肿瘤先导化合物,抗骨质疏松先导化合物和抗菌先导化合物,如PI3K/Tubulin双重抑制剂S9,DNA TopⅡ/Tubulin双重抑制剂YCH337等。

2.领导团队优化得到两个分子靶向抗肿瘤1类新药候选物,其中CYH33国内Ⅰa已经结束,正在进行Ⅰb临床试验,美国IND已获默示许可,盐酸美呋哌瑞的Ⅰ期临床顺利进行中,另有数个化合物在临床前研究阶段。


shrz: 上海市药学会药物化学专业委员会委员

中国抗癌协会抗癌药物专业委员会委员

AACR会员

国际杂环化学学会会员

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