Abstract

Synthesis and biological evaluation of bis-allylidene-4-piperidones analogues

Author(s): Rahul L.Jadhav, Chandrakant S.Magdum

In the view of increasing incidences of cancer and AIDS complication, urgent need of development of the therapeutic agent is required. Recently different series of compounds have been designed which utilized the 1, 5- diaryl -3- oxo- 1, 4- pentadinenyl pharmacophore for development of novel cytotoxic and anticancer agent. The title compounds were prepared by Claisen Schmidt reaction in the basic medium. The resulting synthesized compounds have been screened for in-vitro cytotoxic property by SRBassaymethod against leukemic and colon cancer cell lines. The compounds 1a, 1b & 2b showed equipotent activity against human leukemia cell lines as compared to the standard. The synthesized compounds also screened for HIV-1 protease inhibitor and antimicrobial activity. The compound 2b showed moderate HIV-1 protease inhibitor activity as compared to the standard, pepstatin-A. Antimicrobial activity is due to the presence of á, â-unsaturated carbonyl group. The compound 2 showed significant activity againstA. niger fungi as compared to standard. This study revealed the potential of these molecules for further development as cytotoxic, HIVprotease inhibitor and antifungal agents.