马晓东教授简介

马晓东，复旦大学博士，师从药物化学家陈芬儿院士，从事药物合成开发近15年， 2014年人才引进至大连医科大学药学院，药物化学学科科研骨干，负责创新药物开发平台建设，围绕艾滋病和肿瘤两大领域，已合成筛选500余化合物，并发现明显优于上市药物的新型靶向抗肿瘤分子DY3002（获大连市青年之星项目支持），已完成除安全性评价外的其它临床前研究。申请人以通讯作者在J. Med. Chem.，Acs Med. Chem. Lett., Eur. J. Med. Chem., ChemMedChem, Bioorg. Med. Chem., 等药化期刊发表论文30余篇，申请国际专利1项，中国专利15项，授权7项。主持国家自然科学基金，辽宁省博士启动基金，大连市青年“科技之星”项目。是药学杂志Current Drug Discovery Technologies, Journal of Medical Biotechnology, Clinics in Respiratory Medicine, Journal of Drug Toxicology and Pharmacology, Journal of Oncology Research Forecast,，的国际编委，大连市药学会委员，入选大连市青年科技之星，辽宁省“百千万人才工程”，“兴辽英才计划”青年拔尖人才。
研究方向：
1. 基于计算机辅助药物设计和药物作用机理设计的创新药物开发（靶向抗肿瘤药物）
2. 重大药物及关键医药化工中间体的新工艺开发
3. 手性技术等药物合成新方法研究
发表论文
1. Song, Z., Ge, Y., Wang, C., Huang, S., Shu, X., Liu, K., Zhou, Y., Ma, X*. Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors Against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer. J. Med. Chem. 2016, 59, 6580–94. IF = 6.259  (Q1区)
1. Wang, L., Zhao, J., Yao, Y., Wang, C., Zhang, J., Shu, X., Sun, X., Li, Y., Liu, K., Yun, H., Ma, X*. Covalent binding design strategy: A prospective method for discovery of potent targeted anticancer agents. Eur. J. Med. Chem. 2017, 142, 493-505 . IF = 4.519 (Q1区)
2. Liu, H., Qu, M., Xu, L., Han, X., Wang, C., Shu, X., Yao, J., Liu, K., Peng, J., Li, Y., Ma, X*. Design and synthesis of sulfonamide-substituted diphenylpyrimidines (SFA-DPPYs) as potent Bruton's tyrosine kinase (BTK) inhibitors with improved activity toward B-cell lymphoblastic leukemia. Eur. J. Med. Chem. 2017, 135, 60-69. IF = 4.519 (Q1区);
3. Song, Z., Huang, S., Yu, H., Jiang, Y., Wang, C., Meng, Q., Shu, X., Sun, H., Liu, K., Li, Y., Ma, X*. Synthesis and biological evaluation of morpholine-substituted diphenylpyrimidine derivatives (Mor-DPPYs) as potent EGFR T790M inhibitors with improved activity toward the gefitinib-resistant non-small cell lung cancers (NSCLC). Eur. J. Med. Chem. 2017, 133, 329-339. IF = 4.519 (Q1区)
4. Zhou, J., Huang, Y., Zhang, X., Cheng, Y. *, Tang, L.*, Ma, X*.  Eyes absent gene (EYA1) is a pathogenic driver and a therapeutic target for melanoma. Oncotarget, 2017, 8, 105081-105092. IF  = 5.168 (Q1区).
5. Ge, Y., Wang, C., Song, S., Huang, J., Liu, Z., Li, Y., Meng, Q., Zhang, J., Yao, J., Liu, K., Ma, X*. Sun, X*. Identification of highly potent BTK and JAK3 dual inhibitors with improved activity for the treatment of B-cell lymphoma. Eur. J. Med. Chem. 2018, https://doi.org/10.1016/j.ejmech.2017.10.080 IF = 4.519 (Q1区)
6. Zhao, D., Huang, S., Qu, M., Wang, C., Liu, Z., Li, Z., Peng, J., Liu, K., Li, Y., Ma, X*. Shu, X.* Structural Optimization of Diphenylpyrimidine Derivatives (DPPYs) as Potent Bruton’s Tyrosine Kinase (BTK) Inhibitors with Improved Activity Toward B Leukemia Cell Lines. Eur. J. Med. Chem. 2016, 126, 444–55. IF = 4.519 (Q1区)
7. Yu, H., Li, Y., Ge, Y., Song, Z., Wang, C., Huang, S., Jin, Y., Han, X., Zhen, Y., Liu, K. *, Zhou, Y. *, Ma, X*. Novel 4-Anilinoquinazoline Derivatives Featuring an 1-Adamantyl Moiety as Potent EGFR Inhibitors with Enhanced Activity Against NSCLC Cell Lines. Eur. J. Med. Chem. 2016, 110, 195–203. IF = 4.519 (Q1区)
8. Ge, Y., Jin, Y., Wang, C., Zhang, J., Tang, Z., Peng, J., Liu, K., Li, Y., Zhou, Y., Ma, X*. Discovery of Novel Bruton’s Tyrosine Kinase (BTK) Inhibitors Bearing a N,9-Diphenyl-9H-purin-2-amine Scaffold. ACS Med. Chem. Lett. 2016, 7, 1050–1055. IF = 3.746 (Q1区)
9. Song, A., Zhang, J., Ge, Y., Wang, C., Meng, Q., Tang, Z., Peng, J., Liu, K., Li, Y., Ma, X*. C-2 (E)-4-(Styryl)aniline substituted diphenylpyrimidine derivatives (Sty-DPPYs) as specific kinase inhibitors targeting clinical resistance related EGFRT790M mutant. Bioorg. Med.Chem. 2017, 25, 2724-2729. IF = 2.930.
10. Liu, H., Wu, B., Ge, Y., Huang, J., Song, S., Wang, C., Yao, J., Liu, K., Li, Y., Li, Y. *, Ma, X*. Phosphamide-containing diphenylpyrimidine analogues (PA-DPPYs) as potent focal adhesion kinase (FAK) inhibitors with enhanced activity against pancreatic cancer cell lines. Bioorg. Med. Chem. 2017, 25, 6313-6321. IF = 2.930.

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