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研究员

许恒

职 称:研究员、准聘副教授

所属科室:合成药物化学研究室

导师类别:博士生导师

联系方式:xuheng@www.myhortonhome.com

所属重点实验室:天然药物活性物质与功能国家重点实验室;
活性物质发现与适药化研究北京市重点实验室;
中国医学科学院小分子肿瘤免疫治疗药物重点实验室

个人简介

许恒,bobapp官方下载 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bobapp官方下载 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;2015年9月起任bobapp官方下载 课题组长,主要进行小分子创新药物的设计与研发。

研究方向

1) 抗肿瘤小分子药物设计与研发2) 抗自身免疫性疾病小分子药物设计与研发 3) 基于蛋白靶向降解技术的药物设计与研发 4)光控药物设计与发现

发表论文

(1) 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.
(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 Pharmaceutica Sinica B. https://doi.org/10.1016/j.apsb.2021.05.019.
(3) Sun, Y.#; Fu, R.#; Lin, S.; Zhang, J.; Ji, M.; Zhang, Y.; Wu, D.; Zhang, K.; Tian, H.; Zhang, M.; Sheng, L.; Li, Y.; Jin, J.*; Chen, X.*; Xu, H.* Discovery of New Thieno[2,3-d]pyrimidine and Thiazolo[5,4-d]pyrimidine Derivatives as Orally Active Phosphoinositide 3-Kinase Inhibitors. Bioorg. Med. Chem. 2021, 29, 115890.
(4) 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.
(5) 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.
(6) Wang, L.; Yang, H.; Zang, C.; Dong, Y.; Shang, J.; Chen, J.; Wang, Y.; Liu, H.; Zhang, Z.; Xu, H.*; Bao, X.*; Zhang, D.* CXCR2 antagonism promotes oligodendrocyte precursor cell differentiation and enhances remyelination in a mouse model of multiple sclerosis. Neurobiol. Dis. 2020, 134, 104630.
(7) 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.
(8) 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.
(9) 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.
(10) 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.
(11) 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.
(12) 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.
(13) 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.
(14) 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.
(15) 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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