Design, Synthesis and Antitumoral Activity of New O‐Alkylamidoximes

Abstract

Among poly(ADP-ribose) polymerases (PARPs), PARP-1 has emerged as a target in cancer therapy. The present work was aimed to design and synthesize O-alkylaryl amidoximes as a new antiproliferative agents. The target compounds were designed through the study of molecular docking against the PARP-1 and synthesized from commercially available starting materials in good yields under mild conditions and easy to perform reactions. The synthesized compounds exhibited in vitro antineoplastic activity (0.32-27.8 mM) against MCF-7 and Caco-2 cells, and one of them exhibited selective toxicity when tested against VERO cells. These compounds can be considered good candidates for the next stages in the development of new antiproliferative drugs.