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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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Main Authors: Do, Thi Mai Dung, Eun, Jae Park, Duong, Tien Anh
Format: Bài trích
Language:English
Published: Bentham Science Publishers 2022
Subjects:
Acetohydrazides
Quinazolin-4(3H)-one
Online Access: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

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