Hiển thị ở chế độ nhân viên: Design, Synthesis and Evaluation of Novel (E)-N'-((1-(4-chlorobenzyl)-1H-indol-3-yl)methylene)-2-(4-oxoquinazolin-3(4H)-yl)acetohydrazides as Antitumor Agents

Design, Synthesis and Evaluation of Novel (E)-N'-((1-(4-chlorobenzyl)-1H-indol-3-yl)methylene)-2-(4-oxoquinazolin-3(4H)-yl)acetohydrazides as Antitumor Agents

A biological evaluation revealed that all thirteen compounds designed and synthesized showed strong cytotoxicity against three human cancer cell lines (SW620, colon cancer; PC-3, prostate cancer; NCI-H23, lung cancer) with eight compounds (5a, 5c-i, 5k), which were clearly more potent than both PAC-...

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Tác giả chính:	Do, Thi Mai Dung, Eun, Jae Park, Duong, Tien Anh
Định dạng:	Bài trích
Ngôn ngữ:	English
Nhà xuất bản:	Bentham Science Publishers 2022
Chủ đề:	Acetohydrazides Quinazolin-4(3H)-one
Truy cập trực tuyến:	https://www.eurekaselect.com/article/120263 https://dlib.phenikaa-uni.edu.vn/handle/PNK/5864 https://doi.org/10.2174/1871520622666220118154914
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spelling	oai:localhost:PNK-58642022-08-17T05:54:53Z Design, Synthesis and Evaluation of Novel (E)-N'-((1-(4-chlorobenzyl)-1H-indol-3-yl)methylene)-2-(4-oxoquinazolin-3(4H)-yl)acetohydrazides as Antitumor Agents Do, Thi Mai Dung Eun, Jae Park Duong, Tien Anh Acetohydrazides Quinazolin-4(3H)-one A biological evaluation revealed that all thirteen compounds designed and synthesized showed strong cytotoxicity against three human cancer cell lines (SW620, colon cancer; PC-3, prostate cancer; NCI-H23, lung cancer) with eight compounds (5a, 5c-i, 5k), which were clearly more potent than both PAC-1 and oncrasin-1. In this series, four compounds, including 5c, 5e, 5f, and 5h, were the most potent members with approximately 4- to 5-fold stronger than the reference compounds PAC-1 and oncrasin-1 in terms of IC50. In comparison to 5-FU, these compounds were even 18- to 29-fold more potent in terms of cytotoxicity in three human cell lines tested. In the caspase activation assay, the caspase activity was activated to 285% by compound 5e compared to PAC-1, the first procaspase activating compound, which was used as a control. Our docking simulation revealed that compound 5e was a potent allosteric inhibitor of procaspase-3 through chelation of inhibitory zinc ion. Physicochemical and ADMET calculations for 5e provided useful information of its suitable absorption profile and some toxicological effects that need further optimization to be developed as a promising anticancer agent. 2022-07-13T01:59:44Z 2022-07-13T01:59:44Z 2022 Bài trích https://www.eurekaselect.com/article/120263 https://dlib.phenikaa-uni.edu.vn/handle/PNK/5864 https://doi.org/10.2174/1871520622666220118154914 en Bentham Science Publishers
institution	Digital Phenikaa
collection	Digital Phenikaa
language	English
topic	Acetohydrazides Quinazolin-4(3H)-one
spellingShingle	Acetohydrazides Quinazolin-4(3H)-one Do, Thi Mai Dung Eun, Jae Park Duong, Tien Anh Design, Synthesis and Evaluation of Novel (E)-N'-((1-(4-chlorobenzyl)-1H-indol-3-yl)methylene)-2-(4-oxoquinazolin-3(4H)-yl)acetohydrazides as Antitumor Agents
description	A biological evaluation revealed that all thirteen compounds designed and synthesized showed strong cytotoxicity against three human cancer cell lines (SW620, colon cancer; PC-3, prostate cancer; NCI-H23, lung cancer) with eight compounds (5a, 5c-i, 5k), which were clearly more potent than both PAC-1 and oncrasin-1. In this series, four compounds, including 5c, 5e, 5f, and 5h, were the most potent members with approximately 4- to 5-fold stronger than the reference compounds PAC-1 and oncrasin-1 in terms of IC50. In comparison to 5-FU, these compounds were even 18- to 29-fold more potent in terms of cytotoxicity in three human cell lines tested. In the caspase activation assay, the caspase activity was activated to 285% by compound 5e compared to PAC-1, the first procaspase activating compound, which was used as a control. Our docking simulation revealed that compound 5e was a potent allosteric inhibitor of procaspase-3 through chelation of inhibitory zinc ion. Physicochemical and ADMET calculations for 5e provided useful information of its suitable absorption profile and some toxicological effects that need further optimization to be developed as a promising anticancer agent.
format	Bài trích
author	Do, Thi Mai Dung Eun, Jae Park Duong, Tien Anh
author_facet	Do, Thi Mai Dung Eun, Jae Park Duong, Tien Anh
author_sort	Do, Thi Mai Dung
title	Design, Synthesis and Evaluation of Novel (E)-N'-((1-(4-chlorobenzyl)-1H-indol-3-yl)methylene)-2-(4-oxoquinazolin-3(4H)-yl)acetohydrazides as Antitumor Agents
title_short	Design, Synthesis and Evaluation of Novel (E)-N'-((1-(4-chlorobenzyl)-1H-indol-3-yl)methylene)-2-(4-oxoquinazolin-3(4H)-yl)acetohydrazides as Antitumor Agents
title_full	Design, Synthesis and Evaluation of Novel (E)-N'-((1-(4-chlorobenzyl)-1H-indol-3-yl)methylene)-2-(4-oxoquinazolin-3(4H)-yl)acetohydrazides as Antitumor Agents
title_fullStr	Design, Synthesis and Evaluation of Novel (E)-N'-((1-(4-chlorobenzyl)-1H-indol-3-yl)methylene)-2-(4-oxoquinazolin-3(4H)-yl)acetohydrazides as Antitumor Agents
title_full_unstemmed	Design, Synthesis and Evaluation of Novel (E)-N'-((1-(4-chlorobenzyl)-1H-indol-3-yl)methylene)-2-(4-oxoquinazolin-3(4H)-yl)acetohydrazides as Antitumor Agents
title_sort	design, synthesis and evaluation of novel (e)-n'-((1-(4-chlorobenzyl)-1h-indol-3-yl)methylene)-2-(4-oxoquinazolin-3(4h)-yl)acetohydrazides as antitumor agents
publisher	Bentham Science Publishers
publishDate	2022
url	https://www.eurekaselect.com/article/120263 https://dlib.phenikaa-uni.edu.vn/handle/PNK/5864 https://doi.org/10.2174/1871520622666220118154914
_version_	1751856284664070144
score	8.891145

Design, Synthesis and Evaluation of Novel (E)-N'-((1-(4-chlorobenzyl)-1H-indol-3-yl)methylene)-2-(4-oxoquinazolin-3(4H)-yl)acetohydrazides as Antitumor Agents

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