Synthesis and anticancer properties of 3-furan-2-yl-2-(4-furan/thiophen-2-ylthiazol-2-yl)acrylonitrile derivatives

Abstract

By the reaction of (4-furan-2-yl-thiazol-2-yl)- 3a and (4-thiophen-2-yl-thiazol-2-yl)- 3b acetonitriles with furfural 4 and 5-arylfurfyrals 5a-g 3-furan-2-yl-2-(4-furan/thiophen-2-ylthiazol-2-yl)acrylonitrile derivatives 6a-i were obtained. Anticancer activity screening was carried out within the framework of Developmental Therapeutic Program of the National Cancer Institute's (DTP, NCI, Bethesda, Maryland, USA). It was found out that (2E)-3-(2-furyl)-2-[4-(2-furyl)-1,3-thiazol-2-yl]acrylonitrile (6a) and 2-(4-thiophen-2-yl-thiazol-2-yl)-acrylonitriles 6h,i possessed low activity and 2-(4-furan-2-yl-thiazol-2-yl)acrylonitrile derivatives 6b-g showed moderate action. Compounds 6b-g were sensitive to cell lines of MDA-MB-468 and T-47D Breast Cancer. In this case cytotoxic effect was observed with a range of GP = -38.24 – 1.28%.