Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety

We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed...

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Detalles Bibliográficos
Autores principales: Zhang, Jun, Shen, Weiyi, Li, Xiaoning, Chai, Yun, Li, Senjun, Lv, Kai, Guo, Huiyuan, Liu, Mingliang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2016
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6274105/
https://www.ncbi.nlm.nih.gov/pubmed/27929442
http://dx.doi.org/10.3390/molecules21121674
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author Zhang, Jun
Shen, Weiyi
Li, Xiaoning
Chai, Yun
Li, Senjun
Lv, Kai
Guo, Huiyuan
Liu, Mingliang
author_facet Zhang, Jun
Shen, Weiyi
Li, Xiaoning
Chai, Yun
Li, Senjun
Lv, Kai
Guo, Huiyuan
Liu, Mingliang
author_sort Zhang, Jun
collection PubMed
description We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed that some compounds exhibit broad-spectrum antitumor potency, and the most active compound 23p (IC(50): 2.357–3.012 μM) was found more potent than Sunitinib (IC(50): 31.594–49.036 μM) against HepG2, A549 and Skov-3, respectively.
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spelling pubmed-62741052018-12-28 Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety Zhang, Jun Shen, Weiyi Li, Xiaoning Chai, Yun Li, Senjun Lv, Kai Guo, Huiyuan Liu, Mingliang Molecules Article We report herein the design and synthesis of a series of novel 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1H-pyrrole-3-carboxamide moiety. These newly synthesized derivatives were evaluated for in vitro activity against selected cancer cell lines by MTT assay. Results revealed that some compounds exhibit broad-spectrum antitumor potency, and the most active compound 23p (IC(50): 2.357–3.012 μM) was found more potent than Sunitinib (IC(50): 31.594–49.036 μM) against HepG2, A549 and Skov-3, respectively. MDPI 2016-12-06 /pmc/articles/PMC6274105/ /pubmed/27929442 http://dx.doi.org/10.3390/molecules21121674 Text en © 2016 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 (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Zhang, Jun
Shen, Weiyi
Li, Xiaoning
Chai, Yun
Li, Senjun
Lv, Kai
Guo, Huiyuan
Liu, Mingliang
Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety
title Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety
title_full Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety
title_fullStr Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety
title_full_unstemmed Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety
title_short Synthesis and Antitumor Activity of 5-Bromo-7-azaindolin-2-one Derivatives Containing a 2,4-Dimethyl-1H-pyrrole-3-carboxamide Moiety
title_sort synthesis and antitumor activity of 5-bromo-7-azaindolin-2-one derivatives containing a 2,4-dimethyl-1h-pyrrole-3-carboxamide moiety
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6274105/
https://www.ncbi.nlm.nih.gov/pubmed/27929442
http://dx.doi.org/10.3390/molecules21121674
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