N'-[(E)-arylidene]-2-(2,3-dihydro-3-oxo-4H-1,4-benzoxazin-4-yl)-acetohydrazides: synthesis and evaluation of caspase activation activity and cytotoxicity

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Title
N'-[(E)-arylidene]-2-(2,3-dihydro-3-oxo-4H-1,4-benzoxazin-4-yl)-acetohydrazides: synthesis and evaluation of caspase activation activity and cytotoxicity
Author(s)
L C Huan; L C Truc; C V Phuong; P T Hai; L T T Huong; N T P Linh; N T Thuan; E J Park; Y J Choi; Jong Soon Kang; S B Han; N H Nam; P T Tran
Bibliographic Citation
Chemistry & Biodiversity, vol. 15, no. 10, pp. e1800322-e1800322
Publication Year
2018
Abstract
In our search for novel small cytotoxic molecules potentially activating procaspase-3, we have designed and synthesized a series of novel N′-[(E)-arylidene]-2-(2,3-dihydro-3-oxo-4H-1,4-benzoxazin-4-yl)acetohydrazides (5, 6). Biological evaluation revealed that seven compounds, including 5h, 5j, 5k, 5l, 5n, 6a, and 6b, exhibited moderate to strong cytotoxicity against three human cancer cell lines (SW620, colon cancer; PC-3, prostate cancer; NCI-H23, lung cancer). Among these compounds, two most cytotoxic compounds (5h and 5j) displayed from 3- up to 10-fold higher potency than PAC-1 and 5-FU in three cancer cell lines tested. Three compounds 5j, 5k, and 5n were also found to display better caspases activation activity in comparison to PAC-1. Especially, compound 5k activated the level of caspases activity by 200% higher than that of PAC-1. From this study, three compounds 5j, 5k, and 5n could be considered as potential leads for further design and development of caspase activators and anticancer agents.
Keyword
1,4-benzoxazineacetohydrazidescaspase activationcytotoxic activities
ISSN
1612-1872
Publisher
Wiley
DOI
http://dx.doi.org/10.1002/cbdv.201800322
Type
Article
Appears in Collections:
Ochang Branch Institute > Division of National Bio-Infrastructure > Laboratory Animal Resource & Research Center > 1. Journal Articles
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