New acetohydrazides incorporating 2-oxoindoline and 4-oxoquinazoline: synthesis and evaluation of cytotoxicity and caspase activation activity

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Title
New acetohydrazides incorporating 2-oxoindoline and 4-oxoquinazoline: synthesis and evaluation of cytotoxicity and caspase activation activity
Author(s)
L C Huan; D T Anh; B X Truong; P H Duc; P T Hai; L Duc-Anh; L T T Huong; E J Park; H J Lee; Jong Soon Kang; P T Tran; D T T Hai; D T K Oanh; S B Han; N H Nam
Bibliographic Citation
Chemistry & Biodiversity, vol. 17, pp. e1900670-e1900670
Publication Year
2020
Abstract
In our search for new small molecules activating procaspase-3, we have designed and synthesized a series of new acetohydrazides incorporating both 2-oxoindoline and 4-oxoquinazoline scaffolds. Biological evaluation showed that a number of these acetohydrazides were comparably or even more cytotoxic against three human cancer cell lines (SW620, colon cancer; PC-3, prostate cancer; NCI?H23, lung cancer) in comparison to PAC-1, a first procaspase-3 activating compound, which was used as a positive control. One of those new compounds, 2-(6-chloro-4-oxoquinazolin-3(4H)-yl)-N′-[(3Z)-5-methyl-2-oxo-1,2-dihydro-3H-indol-3-ylidene]acetohydrazide activated the caspase-3 activity in U937 human lymphoma cells by 5-fold higher than the untreated control. Three of the new compounds significantly induced necrosis and apoptosis in U937 cells.
Keyword
acetohydrazidescaspase activationcytotoxicityquinazolin-4(3H)-one
ISSN
1612-1872
Publisher
Wiley
DOI
http://dx.doi.org/10.1002/cbdv.201900670
Type
Article
Appears in Collections:
Ochang Branch Institute > Division of Bioinfrastructure > Laboratory Animal Resource Center > 1. Journal Articles
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