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许恒

时间:2020/7/17 来源: 阅读:11599次


许恒

许恒,中国医学科学院药物研究所研究员,博士生导师。1998年本科毕业于南京大学化学系;2005年获得美国德克萨斯大学阿灵顿分校博士学位; 2005年至2008年在美国国立卫生研究院/国家癌症研究所从事博士后研究;2008年至2011年在葛兰素史克中国研发中心工作,担任Senior Scientist从事中枢神经领域新药研究;2011年至2015年在方正医药研究院担任副院长开展创新药物研发工作;20159月起中国医学科学院药物研究所课题组长。

 

联系方式E-mail: xuheng@imm.ac.cn; Tel: 010-83161089

北京市西城区南纬路甲2号,中国医学科学院&北京协和医学院 药物研究所

100050

 

研究方向:小分子药物发现, 当前针对的药物靶点主要集中在肿瘤和自身免疫性疾病领域。

 

近年代表性论文

1. Dong, Y#; Chen, J.#; Cui, Y.; Bao, L.; Xu, H.* Cp*RhIII-catalyzed sulfonamide directed ortho arene C–H carbenoid functionalization with pyridotriazoles. Org. Lett., 2020, 22, 772-775.

2. Lin, S.#; Jin, J.#; Liu, Y.#; Tian, H.; Zhang, Y.; Fu, R.; Zhang, J.; Wang, M.; Du, T.; Ji, M.; Wu, D.; Zhang, K.; Sheng, L.; Li, Y.; Chen, X.*; Xu, H.* Discovery of 4-Methyl Quinazoline Based PI3K Inhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis. J. Med. Chem. 2019, 62, 8873-8879.

3. Zhang, K.#; Lai, F.#; Lin, S.; Ji, M.; Zhang, J.; Zhang, Y.; Jin, J.; Fu, R.; Wu, D.; Tian, H.; Xue, N.; Sheng, L.; Zou, X.; Li, Y.; Chen, X.*; Xu, H.* Design, Synthesis and Biological Evaluation of 4-Methyl Quinazoline Derivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide 3-Kinases and Histone Deacetylases. J. Med. Chem. 2019, 62, 6992-7014.

4. Dong, Y.#; Zhang, X.#; Chen, J.; Zou, W.; Lin, S.; Xu, H.* Switching the site-selectivity of C–H activation in aryl sulfonamides containing strongly coordinating N-heterocycles. Chem. Sci., 2019, 10, 8744-8751.

5. Dong, Y.; Chen, J.; Xu, H.* Rhodium(III)-catalyzed sulfonamide directed ortho C–H carbenoid functionalization via metal carbene migratory insertion. Chem.Commun. 2019, 55, 2027-2030.

6. Lin, S.#; Wang, C.#; Ji, M.; Wu, D.; Lv, Y.; Zhang, K.; Dong, Y.; Jin, J.; Chen, J.; Zhang, J.; Sheng, L.; Li, Y.; Chen, X.*; Xu, H.* Discovery and Optimization of 2-Amino-4-methylquinazoline Derivatives as Highly Potent Phosphatidylinositol 3-kinase Inhibitors for Cancer Treatment. J. Med. Chem. 2018, 61, 6087–6109.

7. Dong, Y.#; Chen, J.#; Xu, H.* Rhodium(III)-catalyzed directed amidation of unactivated C(sp3)–H bonds to afford 1,2-amino alcohol derivatives. Chem. Commun. 2018, 54, 11096-11099.

8. Lin, S.#; Wang, C.#; Ji, M.; Wu, D.; Lv, Y.; Sheng, L.; Han, F.; Dong, Y.; Zhang, K.; Yang, Y.; Li, Y.; Chen, X.*; Xu, H.* Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors. Bioorg. Med. Chem. 2018, 26, 637-646.

9. Xu, H.*; Lu, H.; Xu, Z.; Luan, L.; Li, C.; Xu, Y.; Dong, K.; Zhang, J.; Li, X.; Li, Y.; Gong, S.; Zhao, Y.; Liu, A.; Zhang, Y.; Zhang, W.; Cai, X.; Xiang, J.; Elliott, J. D.; Lin, X.* Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders. ACS Med. Chem. Lett. 2016, 7, 397-402.

10. Han, F.#; Lin, S.#; Liu, P.; Liu, X.; Tao, J.; Deng, X.; Yi, C.; Xu, H.* Discovery of a novel thienopyrimidine series as highly potent and selective PI3K inhibitors. ACS Med. Chem. Lett. 2015, 6, 434-438.

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