Synthesis and Biological Evaluation of Novel N-Methyl-picolinamide-4-thiol Derivatives as Potential Antitumor Agents

A novel series of N-methylpicolinamide-4-thiol derivatives were synthesized and evaluated on human cancer cell lines. Among them, compound 6p displayed potent and broad-spectrum anti-proliferative activities in vitro on some human cancer cell lines, even better than sorafenib. The advanced kinase in...

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Autores principales: Huang, Ting-Ting, Huang, Yun-Chuang, Qing, Xiao- Yu, Xia, Yong, Luo, Xun, Ye, Ting-Hong, Yu, Luo-Ting
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268926/
https://www.ncbi.nlm.nih.gov/pubmed/22634842
http://dx.doi.org/10.3390/molecules17066317
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author Huang, Ting-Ting
Huang, Yun-Chuang
Qing, Xiao- Yu
Xia, Yong
Luo, Xun
Ye, Ting-Hong
Yu, Luo-Ting
author_facet Huang, Ting-Ting
Huang, Yun-Chuang
Qing, Xiao- Yu
Xia, Yong
Luo, Xun
Ye, Ting-Hong
Yu, Luo-Ting
author_sort Huang, Ting-Ting
collection PubMed
description A novel series of N-methylpicolinamide-4-thiol derivatives were synthesized and evaluated on human cancer cell lines. Among them, compound 6p displayed potent and broad-spectrum anti-proliferative activities in vitro on some human cancer cell lines, even better than sorafenib. The advanced kinase inhibitory assays showed that compound 6p could selectively inhibit Aurora-B kinase. The biological results were rationalized by the molecular docking study, which indicated the stable interactions of 6p with the Aurora-B kinase.
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spelling pubmed-62689262018-12-12 Synthesis and Biological Evaluation of Novel N-Methyl-picolinamide-4-thiol Derivatives as Potential Antitumor Agents Huang, Ting-Ting Huang, Yun-Chuang Qing, Xiao- Yu Xia, Yong Luo, Xun Ye, Ting-Hong Yu, Luo-Ting Molecules Article A novel series of N-methylpicolinamide-4-thiol derivatives were synthesized and evaluated on human cancer cell lines. Among them, compound 6p displayed potent and broad-spectrum anti-proliferative activities in vitro on some human cancer cell lines, even better than sorafenib. The advanced kinase inhibitory assays showed that compound 6p could selectively inhibit Aurora-B kinase. The biological results were rationalized by the molecular docking study, which indicated the stable interactions of 6p with the Aurora-B kinase. MDPI 2012-05-25 /pmc/articles/PMC6268926/ /pubmed/22634842 http://dx.doi.org/10.3390/molecules17066317 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Huang, Ting-Ting
Huang, Yun-Chuang
Qing, Xiao- Yu
Xia, Yong
Luo, Xun
Ye, Ting-Hong
Yu, Luo-Ting
Synthesis and Biological Evaluation of Novel N-Methyl-picolinamide-4-thiol Derivatives as Potential Antitumor Agents
title Synthesis and Biological Evaluation of Novel N-Methyl-picolinamide-4-thiol Derivatives as Potential Antitumor Agents
title_full Synthesis and Biological Evaluation of Novel N-Methyl-picolinamide-4-thiol Derivatives as Potential Antitumor Agents
title_fullStr Synthesis and Biological Evaluation of Novel N-Methyl-picolinamide-4-thiol Derivatives as Potential Antitumor Agents
title_full_unstemmed Synthesis and Biological Evaluation of Novel N-Methyl-picolinamide-4-thiol Derivatives as Potential Antitumor Agents
title_short Synthesis and Biological Evaluation of Novel N-Methyl-picolinamide-4-thiol Derivatives as Potential Antitumor Agents
title_sort synthesis and biological evaluation of novel n-methyl-picolinamide-4-thiol derivatives as potential antitumor agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268926/
https://www.ncbi.nlm.nih.gov/pubmed/22634842
http://dx.doi.org/10.3390/molecules17066317
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