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.#; 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 PI3KInhibitors for the Potential Treatment of Idiopathic Pulmonary Fibrosis. J. Med. Chem. 2019, 62, 8873-8879. (# Co-First Authors；封面文章)

2.      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 andoptimization of 2-amino-4-methylquinazoline derivatives as highly potentphosphatidylinositol 3-kinase inhibitors for cancer treatment. J. Med. Chem. 2018, 61, 6087–6109. (# Co-First Authors)

3.      Lin, S.#; Li, Y.#;Zheng, Y.; Luo, L.; Sun, Q.*; Ge, Z.; Cheng, T.; Li, R.* Design, synthesis andbiological evaluation of quinazoline–phosphoramidate mustard conjugates asanticancer drugs. Eur. J. Med. Chem.2017, 127, 442-458 (# Co-First Authors)

4.      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 efficaciousphosphoinositide 3-kinase inhibitors. Bioorg.Med. Chem. 2018, 26,637–646. (# Co-FirstAuthors)

5.      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 andselective PI3K inhibitors. ACS Med.Chem. Lett., 2015, 6,434-438. (# Co-First Authors)

6.      Lin, S.#; Han, F.#; Liu, P.; Tao, J.;Zhong, X.; Liu, X.; Yi, C.*; Xu, H.* Identification of novel7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potentPI3K/mTOR dual inhibitors. Bioorg.Med. Chem. Lett. 2014, 24,790-793. (# Co-First Authors)

7.      Han, F.#;Lin, S.#; Liu, P.; Tao, J.; Yi, C.*; Xu, H.* Synthesis andstructure–activity relationships of PI3K/mTOR dual inhibitors from a series of2-amino-4-methylpyrido[2,3-d]pyrimidine derivatives. Bioorg. Med. Chem. Lett. 2014, 24, 4538-4541. (# Co-First Authors)

8.      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-typedspiro cyclic quaternary ammoniums. Med.Chem. Res. 2014, 23,862-869.

9.      Liang, L.#; Lin, S.#; Lu, J.; Yang, T.; Xiang, Y.; Li, R.*; Zhang,Q.* Novel cathepsin B-sensitive paclitaxel conjugate: Higher water solubility,better efficacy and lower toxicity. J. Control. Release 2012, 160,618-629. (# Co-First Authors)

10.   Lin, S.; Sun, Q.; Ye, J.; Wang, X.; Ge, Z.; Li, R.* Synthesisand structure-analgesic activity relationships of a novel series ofmonospirocyclopiperazinium salts (MSPZ). Bioorg.Med. Chem. Lett. 2011, 21,940-943.

11.   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.

12.   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 agentS-40 targets the colchicine-binding site and shows potent antitumor activity. Cancer Lett. 2020, 495, 22–32.

13.   Xia, L.; Zhang, Y.; Zhang, J.; Lin, S.;Zhang, K.; Tian, H.; Dong, Y.*; Xu, H.* Identification of novelthiazolo[5,4-b]pyridine derivatives as potent phosphoinositide 3-kinaseinhibitors. Molecules 2020, 25, 4630

14.   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.

15.   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 of4-methyl quinazoline derivatives as anticancer agents simultaneously targetingphosphoinositide 3-kinases and histone deacetylases. J. Med. Chem. 2019,62, 6992-7014

16.   Lv, Y.; Du, T.; Ji, M.; Wang, C.; Lin, S.;Xue, N.; Jin, J.; Xu, H.; Chen, X. A novel PI3K/mTOR dual inhibitor XH002exhibited robust antitumor activity in NSCLC. J. Drug Target. 2019,27, 451-459

17.   Chen, Y.; Ji, M.; Zhang ,S.; Xue, N.; Xu, H.; Lin,S.; Chen, X. Bt354 as a new STAT3 signaling pathway inhibitor againsttriple negative breast cancer. J.Drug Target. 2018, 26,920-930.

18.   Zheng, Y.; Zou, W.; Luo, L.; Chen, J.; Lin, S.; Sun, Q.* Ligand-freeCu-catalyzed O-arylation of aliphatic diols. RSC Adv. 2015, 5,66104-66108.