Investigating the Anticancer Activity of Isatin/Dihydropyrazole Hybrids
Meleddu, Rita;Distinto, Simona
;Arridu, Antonella;SERUSI, LORENZO;Cottiglia, Filippo;Deplano, Serenella;Fois, Benedetta;Maccioni, Elias
2019-01-01
Abstract
A series of isatin-dihydropyrazole hybrids have been synthesized in order to assess their potential as anticancer agents. In particular, 12 compounds were evaluated for their antiproliferative activity toward A549, IGR39, U87, MDA-MB-231, MCF-7, BT474, BxPC-3, SKOV-3, and H1299 cell lines, and human foreskin fibroblasts. Four compounds exhibited interesting antiproliferative activity and were further examined to determine their EC 50 values toward a panel of selected tumor cell lines. The best compounds were then investigated for their induced mechanism of cell death. Preliminary structure-activity relationship indicates that the presence of a substituent such as a chlorine atom or a methyl moiety in position 5 of the isatin nucleus is beneficial for the antitumor activity. EMAC4001 proved the most promising compound within the studied series with EC 50 values ranging from 0.01 to 0.38 μM.File | Dimensione | Formato | |
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58-meleddu2018.pdf Open Access dal 19/12/2019
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