Design, Synthesis and Antiproliferative Activity of Novel 2-Substituted-4-amino-6-halogenquinolines

Two series of novel 2-substituted-4-amino-6-halogenquinolines 8a–l and 13a–h were designed, synthesized and evaluated for their antiproliferative activity against H-460, HT-29, HepG2 and SGC-7901 cancer cell lines in vitro. The pharmacological results indicated that most compounds with 2-arylvinyl s...

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Autores principales: Jiang, Nan, Zhai, Xin, Li, Ting, Liu, Difa, Zhang, Tingting, Wang, Bin, Gong, Ping
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268466/
https://www.ncbi.nlm.nih.gov/pubmed/22592090
http://dx.doi.org/10.3390/molecules17055870
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author Jiang, Nan
Zhai, Xin
Li, Ting
Liu, Difa
Zhang, Tingting
Wang, Bin
Gong, Ping
author_facet Jiang, Nan
Zhai, Xin
Li, Ting
Liu, Difa
Zhang, Tingting
Wang, Bin
Gong, Ping
author_sort Jiang, Nan
collection PubMed
description Two series of novel 2-substituted-4-amino-6-halogenquinolines 8a–l and 13a–h were designed, synthesized and evaluated for their antiproliferative activity against H-460, HT-29, HepG2 and SGC-7901 cancer cell lines in vitro. The pharmacological results indicated that most compounds with 2-arylvinyl substituents exhibited good to excellent antiproliferative activity. Among them, compound 8e was a considered promising lead for further structural modifications with IC(50) values of 0.03 μM, 0.55 μM, 0.33 μM and 1.24 μM, which was 2.5- to 186-fold more active than gefitinib and compound 1.
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spelling pubmed-62684662018-12-20 Design, Synthesis and Antiproliferative Activity of Novel 2-Substituted-4-amino-6-halogenquinolines Jiang, Nan Zhai, Xin Li, Ting Liu, Difa Zhang, Tingting Wang, Bin Gong, Ping Molecules Article Two series of novel 2-substituted-4-amino-6-halogenquinolines 8a–l and 13a–h were designed, synthesized and evaluated for their antiproliferative activity against H-460, HT-29, HepG2 and SGC-7901 cancer cell lines in vitro. The pharmacological results indicated that most compounds with 2-arylvinyl substituents exhibited good to excellent antiproliferative activity. Among them, compound 8e was a considered promising lead for further structural modifications with IC(50) values of 0.03 μM, 0.55 μM, 0.33 μM and 1.24 μM, which was 2.5- to 186-fold more active than gefitinib and compound 1. MDPI 2012-05-16 /pmc/articles/PMC6268466/ /pubmed/22592090 http://dx.doi.org/10.3390/molecules17055870 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
Jiang, Nan
Zhai, Xin
Li, Ting
Liu, Difa
Zhang, Tingting
Wang, Bin
Gong, Ping
Design, Synthesis and Antiproliferative Activity of Novel 2-Substituted-4-amino-6-halogenquinolines
title Design, Synthesis and Antiproliferative Activity of Novel 2-Substituted-4-amino-6-halogenquinolines
title_full Design, Synthesis and Antiproliferative Activity of Novel 2-Substituted-4-amino-6-halogenquinolines
title_fullStr Design, Synthesis and Antiproliferative Activity of Novel 2-Substituted-4-amino-6-halogenquinolines
title_full_unstemmed Design, Synthesis and Antiproliferative Activity of Novel 2-Substituted-4-amino-6-halogenquinolines
title_short Design, Synthesis and Antiproliferative Activity of Novel 2-Substituted-4-amino-6-halogenquinolines
title_sort design, synthesis and antiproliferative activity of novel 2-substituted-4-amino-6-halogenquinolines
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6268466/
https://www.ncbi.nlm.nih.gov/pubmed/22592090
http://dx.doi.org/10.3390/molecules17055870
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