A number of diversely functionalized derivatives of a novel [1,3]selenazolo[4,5-d]pyrimidine 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 μM and 533, 390 and 204 μM of IC50 values after 24, 48 and 72 h of treatments, respectively, while they had no significant toxic effects on normal cells.

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