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

Autor: Huan LC; Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, 10000, Vietnam., Anh DT; Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, 10000, Vietnam., Truong BX; Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, 10000, Vietnam., Duc PH; Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, 10000, Vietnam., Hai PT; Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, 10000, Vietnam., Duc-Anh L; Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, 10000, Vietnam., Huong LT; School of Medicine and Pharmacy, Hanoi National University, 144 Xuan Thuy, Hanoi, 10000, Vietnam., Park EJ; College of Pharmacy, Chungbuk National University, 194-31, Osongsaengmyung-1, Heungdeok, Cheongju, Chungbuk, 28160, Republic of Korea., Lee HJ; College of Pharmacy, Chungbuk National University, 194-31, Osongsaengmyung-1, Heungdeok, Cheongju, Chungbuk, 28160, Republic of Korea., Kang JS; Bio-Evaluation Center, Korea Research Institute of Bioscience and Biotechnology, Cheongju, Chungbuk, 28116, Republic of Korea., Tran PT; Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, 10000, Vietnam., Thanh Hai DT; Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, 10000, Vietnam., Kim Oanh DT; Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, 10000, Vietnam., Han SB; College of Pharmacy, Chungbuk National University, 194-31, Osongsaengmyung-1, Heungdeok, Cheongju, Chungbuk, 28160, Republic of Korea., Nam NH; Hanoi University of Pharmacy, 13-15 Le Thanh Tong, Hanoi, 10000, Vietnam.
Jazyk: angličtina
Zdroj: Chemistry & biodiversity [Chem Biodivers] 2020 Mar; Vol. 17 (3), pp. e1900670. Date of Electronic Publication: 2020 Feb 04.
DOI: 10.1002/cbdv.201900670
Abstrakt: 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.
(© 2020 Wiley-VHCA AG, Zurich, Switzerland.)
Databáze: MEDLINE
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