Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents

Molecules

Kaiyong Tang¹  Qingqing Huang¹  Jafeng Zeng²  Guangming Wu²  Jinwen Huang²  Junfang Pan² 

[1]Institute of Drug Discovery and Development, Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, Shanghai 200062, China

[2] E-Mails:

[3]Shanghai Hotmed Sciences Co., Ltd., Shanghai 201201, China

[4] E-Mails:

关键词: celastrol C-6 derivatives;    antitumor activity;    in vitro;    in vivo;   

DOI  :  10.3390/molecules190710177

来源: mdpi

【 摘 要 】

New six C6-celastrol derivatives were designed, synthesized, and evaluated for their in vitro cytotoxic activities against nine human cancer cell lines (BGC-823, H4, Bel7402, H522, Colo 205, HepG2 and MDA-MB-468). The results showed that most of the compounds displayed potent inhibition against BGC823, H4, and Bel7402, with IC₅₀s of 1.84–0.39 μM. The best compound NST001A was tested in an in vivo antitumor assay on nude mice bearing Colo 205 xenografts, and showed significant inhibition of tumor growth at low concentrations. Therefore, celastrol C-6 derivatives are potential drug candidates for treating cancer.

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.