Quinazolinone is a versatile lead molecule for designing potential bioactive
agents. The compounds that have quinazolin-4-ones moiety are associated with
interesting biological activities such as antifungal, antibacterial, antiviral, antitubercular
and anticancer. In view of this we have undertaken synthesis of various thiadiazol
substituted quinazolin-4-(3H)-ones. Novel 3-(1,3,4-thiadiazol-2-yl)-quinazolin-4-(3H)-
ones (5a-5h) were synthesized by reaction of 5-alkyl/aryl substituted 1,3,4-thiadiazoles
with 2-methyl/phenyl-4H-1,3-benzooxazin-4-ones in the presence of pyridine. All the
synthesized compounds were characterized by spectral and physical data. In vitro
anticancer activity of all the synthesized compounds was determined by MTT assay on
HeLa (Human cervical cancer cell) cells. Most active compounds found in vitro studies
were further evaluated for their in vivo activity on Liquid tumor (Ehrlich’s Ascites
Carcinoma; EAC) induced mice. The anticancer activity of compound 5f was found to be
comparable to that of cisplatin against HeLa cells and was also effective in preventing the
growth of tumor in mice as indicated by decrease in progressive gain in body weight as
well as increase in life span when compared to animals of control group.
