Investigation of fatty acid conjugates of 3,5-bisarylmethylene-4-piperidone derivatives as antitumor agents and human topoisomerase-IIα inhibitors

摘要: A series of five 3,5-bisarylidene-4-piperidones designed as analogs curcumin and their twenty fatty acid conjugates were synthesized candidate anticancer agents. The for efficient delivery these compounds at the targeted cancer sites. cytostatic potential was evaluated against three representative cell lines namely murine leukemic L1210 cells, human T-lymphocyte CEM cells cervical HeLa cells. Most found to exhibit significant anti-cancer activity in vitro. QSAR studies indicated electrophilicity towards cellular nucleophiles may have a key role play activity. Representative also tested topoisomerase IIα inhibitory potential, which strong catalytic inhibition enzyme data showed that possessed robust antioxidant multiple analyses. This study prompted significantly lower damage fibroblasts than currently used drug sorafenib wide spectrum action, supplemented with along non-toxic manifestations, certainly augment candidacy novel conjugates.