Two series of 1,3,4-oxadiazole scaffolds (10a-j & 12a-j) were synthesized and comprehensively characterized using IR, NMR and mass spectra. Subsequently, the synthesized compounds underwent screening for anticancer activity against HepG2 and MCF-7 cell lines. All the 20 compounds exhibited substantial anticancer activity with compounds 10b and 10e demonstrating particularly significant activity surpassing that of the standard 5-fluorouracil. Significantly, compound 10b displayed superior efficacy compared to compound 10e, prompting its selection for further in vivo assessment against diethylnitrosamine-induced hepatocellular carcinoma. In in vivo evaluation, compound 10b significantly reduced levels of AST, ALT, ALP and bilirubin in comparison to the positive control group. It also exhibited significant hepatoprotective effects, albeit marginally less potent than standard 5-fluorouracil. These findings underscore the considerable potential of compound 10b as an anticancer agent within the series, suggesting its candidacy for further development and clinical exploration in cancer therapeutics.
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Sonawane et al. (2024) studied this question.
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