In:
Chemistry & Biodiversity, Wiley, Vol. 15, No. 10 ( 2018-10)
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‐4 H ‐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 ( SW 620, 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.
Type of Medium:
Online Resource
ISSN:
1612-1872
,
1612-1880
DOI:
10.1002/cbdv.201800322
Language:
English
Publisher:
Wiley
Publication Date:
2018
detail.hit.zdb_id:
2139001-0
SSG:
12
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