Design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents
In our search for novel small molecules activating procaspase-3, we have designed and synthesized two series of novel (E)-N'-arylidene-2-(2-oxoindolin-1-yl)acetohydrazides (4) and (Z)-2-(5-substituted-2-oxoindolin-1-yl)-N'-(2-oxoindolin-3-ylidene)acetohydrazides (5). Cytotoxic evaluation r...
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Online Access: | https://www.nature.com/articles/s41598-022-06887-0 https://dlib.phenikaa-uni.edu.vn/handle/PNK/5879 https://doi.org/10.1038/s41598-022-06887-0 |
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oai:localhost:PNK-58792022-08-17T05:54:54Z Design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents Do T. M. Dung Eun J. Park Duong T. Anh Dung T. P. Phan Chemical libraries Drug discovery and development In our search for novel small molecules activating procaspase-3, we have designed and synthesized two series of novel (E)-N'-arylidene-2-(2-oxoindolin-1-yl)acetohydrazides (4) and (Z)-2-(5-substituted-2-oxoindolin-1-yl)-N'-(2-oxoindolin-3-ylidene)acetohydrazides (5). Cytotoxic evaluation revealed that the compounds showed notable cytotoxicity toward three human cancer cell lines: colon cancer SW620, prostate cancer PC-3, and lung cancer NCI-H23. Especially, six compounds, including 4f–h and 4n–p, exhibited cytotoxicity equal or superior to positive control PAC-1, the first procaspase-3 activating compound. The most potent compound 4o was three- to five-fold more cytotoxic than PAC-1 in three cancer cell lines tested. Analysis of compounds effects on cell cycle and apoptosis demonstrated that the representative compounds 4f, 4h, 4n, 4o and 4p (especially 4o) accumulated U937 cells in S phase and substantially induced late cellular apoptosis. The results show that compound 4o would serve as a template for further design and development of novel anticancer agents. 2022-07-13T01:59:47Z 2022-07-13T01:59:47Z 2022 Bài trích https://www.nature.com/articles/s41598-022-06887-0 https://dlib.phenikaa-uni.edu.vn/handle/PNK/5879 https://doi.org/10.1038/s41598-022-06887-0 en Springer |
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Chemical libraries Drug discovery and development Do T. M. Dung Eun J. Park Duong T. Anh Dung T. P. Phan Design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents |
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In our search for novel small molecules activating procaspase-3, we have designed and synthesized two series of novel (E)-N'-arylidene-2-(2-oxoindolin-1-yl)acetohydrazides (4) and (Z)-2-(5-substituted-2-oxoindolin-1-yl)-N'-(2-oxoindolin-3-ylidene)acetohydrazides (5). Cytotoxic evaluation revealed that the compounds showed notable cytotoxicity toward three human cancer cell lines: colon cancer SW620, prostate cancer PC-3, and lung cancer NCI-H23. Especially, six compounds, including 4f–h and 4n–p, exhibited cytotoxicity equal or superior to positive control PAC-1, the first procaspase-3 activating compound. The most potent compound 4o was three- to five-fold more cytotoxic than PAC-1 in three cancer cell lines tested. Analysis of compounds effects on cell cycle and apoptosis demonstrated that the representative compounds 4f, 4h, 4n, 4o and 4p (especially 4o) accumulated U937 cells in S phase and substantially induced late cellular apoptosis. The results show that compound 4o would serve as a template for further design and development of novel anticancer agents. |
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Bài trích |
author |
Do T. M. Dung Eun J. Park Duong T. Anh Dung T. P. Phan |
author_facet |
Do T. M. Dung Eun J. Park Duong T. Anh Dung T. P. Phan |
author_sort |
Do T. M. Dung |
title |
Design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents |
title_short |
Design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents |
title_full |
Design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents |
title_fullStr |
Design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents |
title_full_unstemmed |
Design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents |
title_sort |
design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents |
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Springer |
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2022 |
url |
https://www.nature.com/articles/s41598-022-06887-0 https://dlib.phenikaa-uni.edu.vn/handle/PNK/5879 https://doi.org/10.1038/s41598-022-06887-0 |
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1751856316651929600 |
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8.891145 |