赵立明教授课题组2019年科研进展

发布者:系统管理员发布时间:2021-01-04浏览次数:11

2019年,赵立明教授课题组围绕小分子抗肿瘤药物设计合成和有机合成等方面开展了系列研究工作,代表性工作简介如下:

一、 以组蛋白去乙酰化酶抑制belinostat为先导化合物进行结构修饰,合成了系列化合物并进行了抗肿瘤活性筛选;同时撰写了关于组蛋白去乙酰化酶抑制剂方面的研究综述,结果分别发表在Future Medicinal Chemistry和Current Medicinal Chemistry上,具体如下:

1. Zhang, Jie-Huan; Mottamal Madhusoodanan; Jin, Hai-Shan; Guo, Shanchun; Gu, Yan; Wang, Guangdi;* Zhao, Li-Ming.* Design, Synthesis, and Evaluation of Belinostat Analogs as Histone Deacetylase Inhibitors. Future Med. Chem. 2019, 11, 2765-2778.

https://www.future-science.com/doi/10.4155/fmc-2018-0587 

 2. Zhao, Li-Ming;* Zhang, Jie-Huan. Histone Deacetylase Inhibitors in Tumor Immunotherapy. Curr. Med. Chem. 2019, 26, 2990-3008.

https://www.eurekaselect.com/154616/article 

 

二、 围绕1,3-偶极子和氮杂二烯进行了各类环加成反应研究,研究结果分别发表在Chemical Communications,Journal of Organic Chemistry和Advanced Synthesis & Catalysis上,具体如下:

1. Fang, Qing-Yun; Jin, Hai-Shan; Wang, Ru-Bing;* Zhao, Li-Ming.* DABCO-mediated [3+3] cycloaddition of azomethine imines with in situ generated nitrile oxides from hydroximoyl chlorides. Chem. Commun. 2019, 55, 10587-10590.

https://pubs.rsc.org/en/content/articlelanding/2019/cc/c9cc05367k 

 

 

2. Li, De-Feng; Gu, Yan; Zhang, Jing-Ru; Liu, Kun; Zhao, Li-Ming.* Diastereoselective Construction of Spiro-furo[3,2-c]benzopyranoxindoles through a Cu(OTf)2/AcOH Cooperative Promoted Bicyclization Reaction. J. Org. Chem. 2019, 84, 879-887.

https://pubs.acs.org/doi/10.1021/acs.joc.8b02762 

 

3. Zhang, Jing-Ru; Jin, Hai-Shan; Wang, Ru-Bing;* Zhao, Li-Ming.* Synthesis of 2,4-Diaryl-1,3-benzoxazines via FeCl3-Catalyzed Annulation of ortho-Hydroxyphenyl-Substituted para-Quinone Methides with Imidates. Adv. Synth. Catal. 2019, 361, 4811-4816.

https://onlinelibrary.wiley.com/doi/abs/10.1002/adsc.201900842