Novel and versatile methodology for synthesis of cyclic imides and evaluation of their cytotoxic, DNA binding, apoptotic inducing activities and molecular modeling study.
Versatile method has been developed for synthesis of N-substituted imides. Thus, acid anhydrides, imides and dicarboxylic acids were successfully subjected to dehydrative cyclization with substituted amines using DPPOx and Et(3)N to afford N-substituted imides under mild conditions. The DNA binding and apoptosis induction were investigated with regard to their potential utility as cytotoxic agents. Molecular modeling methods are used to study the cytotoxic activity of the active compounds by means of molecular and quantum mechanics.
Abdel-Aziz
Alaa A-M
AA
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia. alaa_moenes@yahoo.com
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D017209:Apoptosis; D004247:DNA / Q000378:metabolism*; D006801:Humans; D007094:Imides / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008958:Models, Molecular; D021281:Quantitative Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D007094:Imides; D004247:DNA