Synthesis and evaluation of 1-(substituted)-3-prop-2-ynylureas as antiangiogenic agents

…, SK Wattanapitayakul, O Prangsaengtong, M Jo…

Index: Sanphanya, Kingkan; Wattanapitayakul, Suvara K.; Prangsaengtong, Orawin; Jo, Michiko; Koizumi, Keiichi; Shibahara, Naotoshi; Priprem, Aroonsri; Fokin, Valery V.; Vajragupta, Opa Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 8 p. 3001 - 3005

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Citation Number: 7

Abstract

Novel urea derivatives of alkynes have been designed, synthesized, and evaluated as potential cancer therapeutics leads. The most active 1-((3-chloromethyl) phenyl)-3-prop-2- ynylurea (1) exhibited cytotoxic effect against HELA and MCF-7 cell lines with IC50 values of 1.55 μM and 1.48 μM, respectively. Further investigation on tube formation assay in human vein umbilical cells (HUVEC) demonstrated that 1 and methyl 4-(3-(3-ethynylureido) ...