Background:
A great array of nitrogen-containing heterocyclic rings were being extensively explored for their functional
versatility in the field of medicine especially in anticancer research. 1,3,4-thiadiazole is one of such heterocyclic ring with promising
anticancer activity against several cancer cell lines, inhibiting diverse biological targets.
Introduction:
The 1,3,4-thiadiazole, when equipped with other heterocyclic scaffolds, has displayed enhanced anticancer properties. The
thiourea, benzothiazole, imidazo[2,1,b][1,3,4]-thiadiazoles are such potential scaffolds with promising anticancer activity.
Method:
A new series of 5-substituted-1,3,4-thiadiazoles linked with phenyl thiourea, benzothiazole and 2,6-disubstituted imidazo[2,1-
b][1,3,4]thiadiazole derivatives were synthesized and tested for in-vitro anticancer activity on various cancer cell lines.
Results:
The National Cancer Institute’s preliminary anticancer screening results showed compounds 4b and 5b having potent antileukemic
activity. Compound 4b selectively showed 32 percent lethality on Human Leukemia-60 cell line. The docking studies of the derivatives on
aromatase enzyme (Protein Data Bank: 3S7S) have shown reversible interactions at the active site with good docking scores comparable to
Letrozole and Exemestane. Further, the selected derivatives were tested for anticancer activity on HeLa cell line based on the molecular
docking studies.
Conclusion:
Compound 4b and 5b showed effective inhibition equivalent to Letrozole. These preliminary biological screening studies have
given positive anticancer activity for these new classes of derivatives. An additional research study like the mechanism of action of the
anticancer activity of this new class of compounds is necessary. These groundwork studies illuminate a future pathway for research of this
class of compounds enabling the discovery of potent antitumor agents.
Design, Synthesis, and In Vitro Antiproliferative Activity of Hydantoin and Purine Derivatives with the 4-Acetylphenylpiperazinylalkyl Moiety
