Synthesis of Various Derivatives of 1,3Selenazolo4,5-dpyrimidine and Exploitation of These Heterocyclic Systems as Antibacterial, Antifungal, and Anticancer Agents

摘要

abstract_textpA number of diversely functionalized derivatives of a novel 1,3selenazolo4,5-dpyrimidine have been synthesized through heterocyclization of some 2,4,5-trisubstituted-1,3-selenazoles with orthoesters in refluxing acetic acid. The synthetic compounds were evaluated for their antimicrobial activity against a panel of microorganisms including Gram-negative bacteria, Gram-positive bacteria, and pathogenic fungi. The antifungal results revealed that the new selenium-containing heterocycles were as good as or sometimes better than terbinafine and fluconazole. The in vitro anticancer activities of aforementioned heterocyclic compounds were screened against human breast carcinoma MCF-7 and HeLa cervical cancer cells as well as HDF (human dermal fibroblast) normal cells. Antiproliferative results indicated that compounds with piperidine moiety on MCF-7 cells and with morpholine moiety on HeLa cells exhibited well broad-spectrum of anticancer activities with 397, 298 and 235 mu M and 533, 390 and 204 mu M of IC(50)values after 24, 48 and 72 h of treatments, respectively, while they had no significant toxic effects on normal cells./p/abstract_text