Synthesis and anti breast cancer activity of biphenyl based chalcones

A series of (2E,2'E)-1,1'-(3-hydroxy-5-methylbiphenyl-2,6-diyl)-bis(3-pheylprop-2-ene-1-ones (5-33) were prepared by the reaction of 1,3-diacetyl biphenyls (1-4) with different aldehydes in presence of catalytic amount of solid KOH in ethanol in excellent yields. The compounds were evaluated for Anticancer activity against human breast Cancer MCF-7 (estrogen responsive proliferative breast Cancer model) and MDA-MB-231 (estrogen independent aggressive breast Cancer model) cell lines, HeLa (cervical Cancer) cell line, and human embryonic kidney (HEK-293) cells. Most of the compounds preferentially inhibited the growth of the aggressive human breast Cancer cell lines, MDA-MB-231 in the range of 4.4-30 μM. The two compounds 9 and 29 proved to be better Anticancer agents than the standard drug tamoxifen against the MDA-MB-231 cell lines. Mode of action of these compounds was established to be Apoptosis, cell cycle arrest and loss of mitochondrial membrane potential.