Design, synthesis, and evaluation of novel N'-substituted-1-(4-chlorobenzyl)-1 H-indol-3-carbohydrazides as antitumor agents

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Title
Design, synthesis, and evaluation of novel N'-substituted-1-(4-chlorobenzyl)-1 H-indol-3-carbohydrazides as antitumor agents
Author(s)
L C Huan; D T Anh; P T Hai; L D Anh; E J Park; A Y Ji; Jong Soon Kang; D T M Dung; D T K Oanh; T T Tung; D T T Hai; S B Han; N H Nam
Bibliographic Citation
Journal of Enzyme Inhibition and Medicinal Chemistry, vol. 35, no. 1, pp. 1854-1865
Publication Year
2020
Abstract
In continuity of our search for novel anticancer agents acting as procaspase activators, we have designed and synthesised two series of (E)-N′-benzylidene-carbohydrazides (4a-m) and (Z)-N'-(2-oxoindolin-3-ylidene)carbohydrazides (5a-g) incorporating 1-(4-chlorobenzyl)-1H-indole core. Bioevaluation showed that the compounds, especially compounds in series 4a-m, exhibited potent cytotoxicity against three human cancer cell lines (SW620, colon cancer; PC-3, prostate cancer; NCI-H23, lung cancer). Within series 4a-m, compounds with 2-OH substituent (4g-i) exhibited very strong cytotoxicity in three human cancer cell lines assayed with IC50 values in the range of 0.56-0.83 μM. In particular, two compounds 4d and 4f bearing 4-Cl and 4-NO2 substituents, respectively, were the most potent in term of cytotoxicity with IC50 values of 0.011-0.001μM. In caspase activation assay, compounds 4b and 4f were found to activate caspase activity by 314.3 and 270.7% relative to PAC-1. This investigation has demonstrated the potential of these simple acetohydrazides, especially compounds 4b, 4d, and 4f, as anticancer agents.
Keyword
Acetohydrazidesisatincytotoxicitycaspase activation
ISSN
1475-6366
Publisher
T&F (Taylor & Francis)
DOI
http://dx.doi.org/10.1080/14756366.2020.1816997
Type
Article
Appears in Collections:
Ochang Branch Institute > Division of Bioinfrastructure > Laboratory Animal Resource Center > 1. Journal Articles
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