Synthesis and Biological Evaluation of 3-Substituted-indolin-2-one Derivatives Containing Chloropyrrole Moieties
Eighteen novel 3-substituted-indolin-2-ones containing chloropyrroles were synthesized and their biological activities were evaluated. The presence of a chlorine atom on the pyrrole ring was crucial to reduce cardiotoxicity. The presence of a 2-(ethyl-amino)ethylcarbamoyl group as a substituent at t...
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Online Access: | http://www.mdpi.com/1420-3049/16/11/9368/ |
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doaj-6b309329dbec41528d3ed435cbaa3b872020-11-24T23:22:12ZengMDPI AGMolecules1420-30492011-11-0116119368938510.3390/molecules16119368Synthesis and Biological Evaluation of 3-Substituted-indolin-2-one Derivatives Containing Chloropyrrole MoietiesRong-Hua ZhangLin XiaoQuan-Hai LiuZhan-Cheng LiNan MaDa-Xu FuYun-Zhou JinEighteen novel 3-substituted-indolin-2-ones containing chloropyrroles were synthesized and their biological activities were evaluated. The presence of a chlorine atom on the pyrrole ring was crucial to reduce cardiotoxicity. The presence of a 2-(ethyl-amino)ethylcarbamoyl group as a substituent at the C-4′ position of the pyrrole enhanced the antitumor activities notably. IC50 values as low as 0.32, 0.67, 1.19 and 1.22 μM were achieved against non-small cell lung cancer (A549), oral epithelial (KB), melanoma (K111) and large cell lung cancer cell lines (NCI-H460), respectively.http://www.mdpi.com/1420-3049/16/11/9368/antitumor activitiesindolin-2-onechloropyrrolesynthesis |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Rong-Hua Zhang Lin Xiao Quan-Hai Liu Zhan-Cheng Li Nan Ma Da-Xu Fu Yun-Zhou Jin |
spellingShingle |
Rong-Hua Zhang Lin Xiao Quan-Hai Liu Zhan-Cheng Li Nan Ma Da-Xu Fu Yun-Zhou Jin Synthesis and Biological Evaluation of 3-Substituted-indolin-2-one Derivatives Containing Chloropyrrole Moieties Molecules antitumor activities indolin-2-one chloropyrrole synthesis |
author_facet |
Rong-Hua Zhang Lin Xiao Quan-Hai Liu Zhan-Cheng Li Nan Ma Da-Xu Fu Yun-Zhou Jin |
author_sort |
Rong-Hua Zhang |
title |
Synthesis and Biological Evaluation of 3-Substituted-indolin-2-one Derivatives Containing Chloropyrrole Moieties |
title_short |
Synthesis and Biological Evaluation of 3-Substituted-indolin-2-one Derivatives Containing Chloropyrrole Moieties |
title_full |
Synthesis and Biological Evaluation of 3-Substituted-indolin-2-one Derivatives Containing Chloropyrrole Moieties |
title_fullStr |
Synthesis and Biological Evaluation of 3-Substituted-indolin-2-one Derivatives Containing Chloropyrrole Moieties |
title_full_unstemmed |
Synthesis and Biological Evaluation of 3-Substituted-indolin-2-one Derivatives Containing Chloropyrrole Moieties |
title_sort |
synthesis and biological evaluation of 3-substituted-indolin-2-one derivatives containing chloropyrrole moieties |
publisher |
MDPI AG |
series |
Molecules |
issn |
1420-3049 |
publishDate |
2011-11-01 |
description |
Eighteen novel 3-substituted-indolin-2-ones containing chloropyrroles were synthesized and their biological activities were evaluated. The presence of a chlorine atom on the pyrrole ring was crucial to reduce cardiotoxicity. The presence of a 2-(ethyl-amino)ethylcarbamoyl group as a substituent at the C-4′ position of the pyrrole enhanced the antitumor activities notably. IC50 values as low as 0.32, 0.67, 1.19 and 1.22 μM were achieved against non-small cell lung cancer (A549), oral epithelial (KB), melanoma (K111) and large cell lung cancer cell lines (NCI-H460), respectively. |
topic |
antitumor activities indolin-2-one chloropyrrole synthesis |
url |
http://www.mdpi.com/1420-3049/16/11/9368/ |
work_keys_str_mv |
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