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Molecules 2014, 19(7), 10177-10188; doi:10.3390/molecules190710177

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

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
Shanghai Hotmed Sciences Co., Ltd., Shanghai 201201, China
*
Authors to whom correspondence should be addressed.
Received: 7 May 2014 / Revised: 2 July 2014 / Accepted: 4 July 2014 / Published: 14 July 2014
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [691 KB, uploaded 16 July 2014]   |  

Abstract

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. View Full-Text
Keywords: celastrol C-6 derivatives; antitumor activity; in vitro; in vivo celastrol C-6 derivatives; antitumor activity; in vitro; in vivo
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MDPI and ACS Style

Tang, K.; Huang, Q.; Zeng, J.; Wu, G.; Huang, J.; Pan, J.; Lu, W. Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents. Molecules 2014, 19, 10177-10188.

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