Design, Synthesis, Molecular Modelling and Anticancer Activities of New Fused Phenanthrolines

Three series of fused pyrrolophenanthroline derivatives were designed as analogues of phenstatin and synthesized in two steps starting with 1,7-phenanthroline, 4,7-phenanthroline and 1,10-phenanthroline, respectively. Two (Compounds and ) of the four compounds tested against a panel of sixty human cancer cell lines of the National Cancer Institute (NCI) exhibited significant growth inhibition activity on several cell lines. Compound showed a broad spectrum in terms of antiproliferative efficacy with GI values in the range of 0.296 to 250 μM. Molecular docking studies indicated that Compounds and are accommodated in the colchicine binding site of tubulin in two different ways.