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药物研究所

个人简介

许恒,1976年生,籍贯山东,中国医学科学院药物研究所研究员,博士生导师,合成药物化学室副主任。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; 2005-2008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;2008-2015年先后在葛兰素史克中国研发中心和方正医药研究院从事新药研发工作;2015年09月起担任中国医学科学院药物研究所课题组长,主要进行小分子创新药物的设计与研发。


主要研究方向

抗肿瘤小分子药物设计与研发;抗自身免疫性疾病小分子药物设计与研发;基于蛋白靶向降解技术的药物设计与研发;光控药物设计与发现。


代表性成果

1. Zhang, J.#; Jiang, H.#; Lin, S.#; Wu, D.; Tian, H.; Jiang, L.; Cui, Y.; Jin, J.*; Chen, X.*; Xu, H.* Design and Optimization of Thienopyrimidine Derivatives as Potent and Selective PI3Kδ Inhibitors for the Treatment of B-Cell Malignancies. J. Med. Chem. 2022, 65, 8011-8028. (IF=8.039)

2. Ji, M.#; Wang, D.#; Lin, S., Wang, C.; Li, L.; Zhang, Z.; Jin, J.; Wu, D.; Dong, Y.; Xu, H.*; Lu, D.*; Chen, X.* A novel PI3K inhibitor XH30 suppresses orthotopic glioblastoma growth and brain metastasis in mice models. Acta Pharm. Sin. B 2022, 12, 774-786. (IF=14.911)

3. Dong, Y.#; Fu, R.#; Chen, J.; Zhang, K.; Ji, M.; Wang, M.; Jiang, H.; Ye, W.; Hu, J.; Li, Y.; Jin, J.*; Chen, X.*; Xu, H.* Discovery of Benzocyclic Sulfone Derivatives as Potent CXCR2 Antagonists for Cancer Immunotherapy. J. Med. Chem. 2021, 64, 16626-16640. (IF=8.039)

4. Zhang, K.#; Ji, M.#; Lin, S.; Peng, S.; Zhang, Z.; Zhang, M.; Zhang, J.; Zhang, Y.; Wu, D.; Tian, H.; Chen, X.*; Xu, H.* Design, Synthesis and Biological Evaluation of a Novel Photocaged PI3K Inhibitor toward Precise Cancer Treatment. J. Med. Chem. 2021, 64, 7331-7340. (IF=8.039)

5. Du, T.; Lin, S.; Ji, M.; Xue, N.; Liu, Y.; Zhang, Z.; Zhang, K.; Zhang, J.; Zhang, Y.; Wang, Q.; Sheng, L.; Li, Y.; Lu, D.*; Chen, X.*; Xu, H.* A novel orally active microtubule destabilizing agent S-40 targets the colchicine-binding site and shows potent antitumor activity. Cancer Lett. 2020, 495, 22-32. (IF=8.679)

6. 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. (IF=6.222)

7. 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. (IF=9.346)

8. 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. (IF=6.205)

9.  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. (IF=6.205)

10. 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. (IF=6.054)