New Acetohydrazides Incorporating 2-Oxoindoline and 4-Oxoquinazoline: Synthesis and Evaluation of Cytotoxicity and Caspase Activation Activity.

New Acetohydrazides Incorporating 2-Oxoindoline and 4-Oxoquinazoline: Synthesis and Evaluation of Cytotoxicity and Caspase Activation Activity. Chem Biodivers. 2020 Jan 13;: Authors: Nam NH, Huan LC, Anh DT, Truong BX, Duc PH, Hai PT, Duc-Anh L, Huong LT, Park EJ, Lee HJ, Kang JS, Tran PT, Oanh DTK, Han SB, Hai DTT Abstract In our search for novel small molecules activating procaspase-3, we have designed and synthesized a series of novel acetohydrazides incorporating both 2-oxoindoline and 4-oxoquinazoline scaffolds (5a-t). 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. Compound 5k activated the caspase-3 activity in U937 human lymphoma cells by 5-fold higher than the untreated control. Three compounds, including 5k, 5n and 5q, significantly induced necrosis and apoptosis in U937 cells. PMID: 31943757 [PubMed - as supplied by publisher]
Source: Chemistry and Biodiversity - Category: Biochemistry Authors: Tags: Chem Biodivers Source Type: research