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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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Main Authors: Dung, Do T. M., Park, Eun J., Anh, Duong T.
Format: Bài trích
Language:English
Published: Springer 2022
Subjects:
Chemical libraries
Drug discovery and development
Online Access:https://www.nature.com/articles/s41598-022-06887-0
https://dlib.phenikaa-uni.edu.vn/handle/PNK/5739
https://doi.org/10.1038/s41598-022-06887-0
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spelling oai:localhost:PNK-57392022-08-17T05:54:52Z Design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents Dung, Do T. M. Park, Eun J. Anh, Duong T. 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. 2022-05-05T07:26:15Z 2022-05-05T07:26:15Z 2022 Bài trích https://www.nature.com/articles/s41598-022-06887-0 https://dlib.phenikaa-uni.edu.vn/handle/PNK/5739 https://doi.org/10.1038/s41598-022-06887-0 en Springer
institution Digital Phenikaa
collection Digital Phenikaa
language English
topic Chemical libraries
Drug discovery and development
spellingShingle Chemical libraries
Drug discovery and development
Dung, Do T. M.
Park, Eun J.
Anh, Duong T.
Design, synthesis and evaluation of novel 2-oxoindoline-based acetohydrazides as antitumor agents
description 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.
format Bài trích
author Dung, Do T. M.
Park, Eun J.
Anh, Duong T.
author_facet Dung, Do T. M.
Park, Eun J.
Anh, Duong T.
author_sort Dung, Do T. M.
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
publisher Springer
publishDate 2022
url https://www.nature.com/articles/s41598-022-06887-0
https://dlib.phenikaa-uni.edu.vn/handle/PNK/5739
https://doi.org/10.1038/s41598-022-06887-0
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score 8.891145

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