1. 工作经历
2011.08-2013.10 北京大学&方正医药研究院,博士后
2015.09-2019.09 中国医学科学院药物研究所,助理研究员
2019.09至今 中国医学科学院药物研究所,副研究员
2. 教育背景
2001.09-2005.07 北京大学药学院,药学,学士
2005.09-2007.07 北京大学药学院,化学生物学,硕士
2007.09-2011.01 北京大学药学院,化学生物学,博士
3. 在研项目
(1)pi3k亚型选择性抑制剂的设计、合成和活性评价
(2)protac分子的设计、合成和活性评价
(3)抗肿瘤药物的靶向递送和释放
以分子靶向药物为主要研究领域,开展小分子靶向抗肿瘤药物和自身免疫性疾病治疗药物等新药研发工作;在此基础上,进行protac分子的设计、合成和活性评价,探索protac技术在各种疾病中的应用;同时,针对肿瘤组织的特殊性,研究抗肿瘤药物的靶向递送和释放技术研究,提高抗肿瘤药物的疗效和安全性。
1. lin, s.#; du, t.#; zhang, j.#; wu, d.; tian, h.; zhang, k.; jiang, l.; lu, d.; sheng, l.; li, 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. (# co-first authors;封面文章)
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. (# co-first authors;封面文章)
3. 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-methylquinazoline based pi3k inhibitors for the potential treatment of idiopathic pulmonary fibrosis. j. med. chem. 2019, 62, 8873-8879. (# co-first authors;封面文章)
4. 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. (# co-first authors)
5. 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. (# co-first authors)
6. lin, s.#; li, y.#; zheng, y.; luo, l.; sun, q.*; ge, z.; cheng, t.; li, r.* design, synthesis and biological evaluation of quinazoline–phosphoramidate mustard conjugates as anticancer drugs. eur. j. med. chem. 2017, 127, 442-458 (# co-first authors)
7. han, f.#; lin, s.#; liu, p.; liu, x.; tao, j.; deng, x.; yi, c.; xu, h.* discovery of a novel series of thienopyrimidine as highly potent and selective pi3k inhibitors. acs med. chem. lett., 2015, 6, 434-438. (# co-first authors)
8. lin, s.#; han, f.#; liu, p.; tao, j.; zhong, x.; liu, x.; yi, c.*; xu, h.* identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1h)-one derivatives as potent pi3k/mtor dual inhibitors. bioorg. med. chem. lett. 2014, 24, 790-793. (# co-first authors)
9. han, f.#; lin, s.#; liu, p.; tao, j.; yi, c.*; xu, h.* synthesis and structure–activity relationships of pi3k/mtor dual inhibitors from a series of 2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives. bioorg. med. chem. lett. 2014, 24, 4538-4541. (# co-first authors)
10. lin, s.; wang, n.; zhao, s.; sun, q.; zhang, w.; ye, j.; cheng, t.; li, r.* synthesis and analgesic evaluation of a series of proline-typed spiro cyclic quaternary ammoniums. med. chem. res. 2014, 23, 862-869.
1. heng xu; xiaoguang chen; songwen lin; ming ji; nina xue; deyu wu; jing jin. benzamide compound and preparation method, use, and pharmaceutical composition thereof. ep patent no.: ep3747866b1; date of patent: 2023-03-01.
2. heng xu; xiaoguang chen; songwen lin; ming ji; jing jin; deyu wu; chunyang wang; yuanhao lv. quinazoline compounds, preparation method, use, and pharmaceutical composition thereof. us patent no.: us11534443b2; date of patent: 2022-12-27.
3. heng xu; xiaoguang chen; songwen lin; ming ji; nina xue; deyu wu; jing jin. benzamide compound and preparation method, use, and pharmaceutical composition thereof. us patent no.: us11518744b2; date of patent: 2022-12-06.
4. heng xu; xiaoguang chen; songwen lin; ming ji; nina xue; deyu wu; jing jin. benzamide compounds and their preparation, use and pharmaceutical compositions. jp patent no.: jp7110362b2; date of patent: 2022-08-01.
5. heng xu; xiaoguang chen; songwen lin; ming ji; jing jin; deyu wu; chunyang wang; yuanhao lv. quinazoline compound and its preparation method, use and pharmaceutical composition. jp patent no.: jp7077323b2; date of patent: 2022-05-30.
6. 许恒,陈晓光,林松文,季鸣,张敬博,杜婷婷。吡唑类化合物及其制备方法、用途和药物组合。中国专利号:zl201811484464.9;授权日:2022-04-15。
7. 许恒,陈晓光,林松文,季鸣,薛妮娜,吴德雨,金晶,陈越。苯甲酰胺类化合物及其制备方法、用途和药物组合物。中国专利号:zl201810090951.0;授权日:2022-03-15。
8. 许恒、陈晓光、林松文、季鸣、金晶、吴德雨、王春阳、吕元皓。喹唑啉类化合物及其制备方法、用途和药物组合物。中国专利号:zl201611214102.9;授权日:2021-07-06。
9. 许恒、陈晓光、林松文、季鸣、吴德雨、王春阳、吕元皓。喹唑啉类化合物及其制备方法、用途和药物组合物。中国专利号:zl201611204309.8;授权日:2021-07-06。
10. 许恒、陈晓光、林松文、季鸣、吴德雨、王春阳、吕元皓。喹唑啉类化合物及其制备方法、用途和药物组合物。中国专利号:zl201611211589.5;授权日:2021-07-02。