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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;2015年9月起任中国医学科学院药物研究所课题组长,主要进行抗肿瘤及抗自身免疫性疾病小分子创新药物的发现研究。
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支持扩展名:.rar .zip .doc .docx .pdf .jpg .png .jpeg(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 PI3KInhibitor 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 andbrain metastasis in mice models. ActaPharmaceutica 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 NewThieno[2,3-d]pyrimidine and Thiazolo[5,4-d]pyrimidine Derivatives as OrallyActive 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 thecolchicine-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 carbenoidfunctionalization 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.* CXCR2antagonism promotes oligodendrocyte precursor cell differentiation and enhancesremyelination 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 forthe 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 QuinazolineDerivatives as Anticancer Agents Simultaneously Targeting Phosphoinositide3-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 sulfonamidescontaining strongly coordinating N-heterocycles. Chem. Sci., 2019, 10, 8744-8751.
(10) Dong, Y.; Chen, J.; Xu, H.* Rhodium(III)-catalyzedsulfonamide directed ortho C–H carbenoid functionalization via metal carbenemigratory 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 HighlyPotent Phosphatidylinositol 3-kinase Inhibitors for Cancer Treatment. J. Med. Chem. 2018, 61, 6087–6109.
(12) Dong, Y.#; Chen, J.#;Xu, H.* Rhodium(III)-catalyzeddirected amidation of unactivated C(sp3)–H bonds to afford 1,2-amino alcoholderivatives. 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 ofnew thienopyrimidine derivatives as potent and orally efficaciousphosphoinositide 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 CXCR2Antagonists 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 highlypotent and selective PI3K inhibitors. ACSMed. Chem. Lett. 2015, 6, 434-438.
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