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，主要进行小分子创新药物的设计与研发。
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
代表性论文：
(1) lin, s.#; du, t. #; zhang, j. #; wu, d.; tian, h.; zhang, k.; jiang, l.; lu, d.; sheng, l.; lin, y.; ji, m.*; chen, x.*; xu, h.* optimization of benzamide derivatives as potent and orally active tubulin inhibitors targeting the colchicine binding site. j. med. chem. 2022, 65, 16372−16391.
(2) 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.
(3) zhang, y.; peng, s.; lin, s.; ji, m.; du, t.*; chen, x.*; xu, h.* discovery of a novel photoswitchable pi3k inhibitor toward optically-controlled anticancer activity. bioorg. med. chem. 2022, 116975.
(4) 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.
(5) 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.
(6) 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.
(7) dong, y. #; mei, b. #; zhang, x.*; xu, h.* selective gram-scale c–h carbenoid functionalization of n-sulfonylarylamides with rhodium catalyst. j. org. chem. 2021, 86, 11660-11672.
(8) 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.
(9) 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.
(10) 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.
(11) 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.
(12) 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.
(13) 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.
(14) 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.
(15) 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.
(16) 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.
