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

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 BGC8...

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Autores principales: Tang, Kaiyong, Huang, Qingqing, Zeng, Jafeng, Wu, Guangming, Huang, Jinwen, Pan, Junfang, Lu, Wei
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271447/
https://www.ncbi.nlm.nih.gov/pubmed/25025148
http://dx.doi.org/10.3390/molecules190710177
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author Tang, Kaiyong
Huang, Qingqing
Zeng, Jafeng
Wu, Guangming
Huang, Jinwen
Pan, Junfang
Lu, Wei
author_facet Tang, Kaiyong
Huang, Qingqing
Zeng, Jafeng
Wu, Guangming
Huang, Jinwen
Pan, Junfang
Lu, Wei
author_sort Tang, Kaiyong
collection PubMed
description 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 IC(50)s 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.
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spelling pubmed-62714472018-12-21 Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents Tang, Kaiyong Huang, Qingqing Zeng, Jafeng Wu, Guangming Huang, Jinwen Pan, Junfang Lu, Wei Molecules Article 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 IC(50)s 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. MDPI 2014-07-14 /pmc/articles/PMC6271447/ /pubmed/25025148 http://dx.doi.org/10.3390/molecules190710177 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Tang, Kaiyong
Huang, Qingqing
Zeng, Jafeng
Wu, Guangming
Huang, Jinwen
Pan, Junfang
Lu, Wei
Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents
title Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents
title_full Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents
title_fullStr Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents
title_full_unstemmed Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents
title_short Design, Synthesis and Biological Evaluation of C(6)-Modified Celastrol Derivatives as Potential Antitumor Agents
title_sort design, synthesis and biological evaluation of c(6)-modified celastrol derivatives as potential antitumor agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271447/
https://www.ncbi.nlm.nih.gov/pubmed/25025148
http://dx.doi.org/10.3390/molecules190710177
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