Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality

Bioorganic & Medicinal Chemistry
Demetrio RaffaGiuseppe Daidone

Abstract

Several new 2-(2-phenoxyacetamido)benzamides 17a-v, 21 and 22 were synthesized by stirring in pyridine the acid chlorides 16a-e and the appropriate5-R-4-R₁-2-aminobenzamide 15a-e and initially evaluated in vitro for antiproliferative activity against the K562 (human chronic myelogenous leukemia) cell line. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). The most active compounds caused an arrest of K562 cells in the G0-G1 phase of cell cycle and induction of apoptosis, which was mediated by caspase activation.

References

May 4, 2004·Il Farmaco·Giuseppe DaidoneMaria Valeria Raimondi
Feb 10, 2009·Chembiochem : a European Journal of Chemical Biology·Teresa SardonIsabelle Vernos
Sep 29, 2011·Journal of Experimental & Clinical Cancer Research : CR·Rebecca S Y Wong
Dec 20, 2014·Cell Death and Differentiation·S ShaliniS Kumar

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Citations

Nov 28, 2015·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Mingyan YangMingan Wang
Jul 4, 2016·European Journal of Medicinal Chemistry·Benedetta MaggioGiuseppe Daidone

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