| Literature DB >> 30996798 |
Rita Meleddu1, Vilma Petrikaite2,3, Simona Distinto1, Antonella Arridu1, Rossella Angius4, Lorenzo Serusi1, Laura Škarnulytė2, Ugnė Endriulaitytė2, Miglė Paškevičiu Tė2, Filippo Cottiglia1, Marco Gaspari5, Domenico Taverna5, Serenella Deplano1, Benedetta Fois1, Elias Maccioni1.
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 EC50 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 EC50 values ranging from 0.01 to 0.38 μM.Entities:
Year: 2018 PMID： 30996798 PMCID： PMC6466827 DOI： 10.1021/acsmedchemlett.8b00596
Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345