Synthesis and anticancer activity of dichloroplatinum(II) complexes of podophyllotoxin

A series of dichloroplatinum(II) complexes of podophyllotoxin (PPT) were prepared, and their cytotoxicity against sensitive (A-549, HeLa, HCT-8, Hep-G2, K562) and resistant (ADM/K562) cell lines were evaluated. Complex cis-[4 alpha-O-(2 '',3 ''-diaminopropanoyl)-podophyllotoxin] dichloride platinum(II) (12) displayed most potent cytotoxicity with IC50 value in the range 0.071-2.98 mu M. Complex 12 induces cell cycle arrest in the G(2)/M phase, and inhibits the formation of microtubules in HeLa cells. Furthermore, this complex exhibits potent DNA cleavage capabilities. (C) 2013 Elsevier Ltd. All rights reserved.