Abstract
A novel series of hybrids of indolin-2-one and quinazolin-4(3H)-one linked via an imine bond were synthesized and tested for their inhibitory activity against the proliferation of a panel of five human cancer cell lines. We found that compound 5c bearing 5-bromo substituent at the indolin-2-one ring exhibited weak cytotoxic activity with percentages of inhibition ranging from 27% to 49% at 20 μM, while its counterpart 7c having 4-methoxybenzyl group at the N1-position of indolin-2-one ring was more active with percentages of inhibition in range of 32-63%. These results indicate that the presence of a bromo substituent at the 5-position and a 4-methoxybenzyl group at the N1-position of indolin-2-one ring is important for the cytotoxic activity.
Keywords: Antitproliferative activity, Hybrid, Indolin-2-one, Quinazolin-4(3H)-one, Synthesis, gastrointestinal stromal tumor, Nolatrexed, 2-Methylquinazolin, nitroquinazolin, MTT Assay
Letters in Drug Design & Discovery
Title:Synthesis and Antiproliferative Evaluation of Hybrids of Indolin-2-one and Quinazoline-4(3H)-one Linked via Imine Bond
Volume: 10 Issue: 1
Author(s): Wei-Yao Wu, Sheng-Li Cao, Bei-Bei Mao, Ji Liao, Zhong-Feng Li, Hao-Bin Song and Xingzhi Xu
Affiliation:
Keywords: Antitproliferative activity, Hybrid, Indolin-2-one, Quinazolin-4(3H)-one, Synthesis, gastrointestinal stromal tumor, Nolatrexed, 2-Methylquinazolin, nitroquinazolin, MTT Assay
Abstract: A novel series of hybrids of indolin-2-one and quinazolin-4(3H)-one linked via an imine bond were synthesized and tested for their inhibitory activity against the proliferation of a panel of five human cancer cell lines. We found that compound 5c bearing 5-bromo substituent at the indolin-2-one ring exhibited weak cytotoxic activity with percentages of inhibition ranging from 27% to 49% at 20 μM, while its counterpart 7c having 4-methoxybenzyl group at the N1-position of indolin-2-one ring was more active with percentages of inhibition in range of 32-63%. These results indicate that the presence of a bromo substituent at the 5-position and a 4-methoxybenzyl group at the N1-position of indolin-2-one ring is important for the cytotoxic activity.
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Wu Wei-Yao, Cao Sheng-Li, Mao Bei-Bei, Liao Ji, Li Zhong-Feng, Song Hao-Bin and Xu Xingzhi, Synthesis and Antiproliferative Evaluation of Hybrids of Indolin-2-one and Quinazoline-4(3H)-one Linked via Imine Bond, Letters in Drug Design & Discovery 2013; 10 (1) . https://dx.doi.org/10.2174/1570180811309010061
DOI https://dx.doi.org/10.2174/1570180811309010061 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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