Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 10, Issue 4, Pages 571-576Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.8b00596
Keywords
Anticancer agents; isatin-dihydropyrazole hybrids; apoptosis inducers
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Funding
- COST action (Multitarget Paradigm for Innovative Ligand Identification in the Drug Discovery Process MuTaLig) [CA15135]
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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 ECso 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 mu M.
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