Abstract
A series of novel substituted 5-phenyl-methyl (Z)-2-(1-amino-2-((1,3,4-oxadiazol-2-yl)thio)ethylidene)hydrazine-1-carboxylate scaffolds 4(a-m) have been synthesized to assess their potential as anti-inflammatory and anticancer agents. The structures of the synthesized derivatives were established by employing 1H- NMR, 13C- NMR, and LC-MS analysis. In particular, thirteen derivatives were evaluated for their in vivo anti-inflammatory activity by making use of carrageenan-induced paw edema in SD rats and in vitro anticancer activity towards the BT474 female breast cancer cell line. Among the tested derivatives, Compound 4f emerged as a key lead and showed significant inhibition in paw edema volume in vivo (81 %), and compound 4e exhibited interesting ability to inhibit cellular proliferation in vitro (IC50=3.78 µM for BT474) compared to Doxorubicin (IC50 = 6.795 μM). Based on the structure-activity relationship, the presence of electron-donating substituents along with oxadiazole nucleus seems favorable for biological activities. A docking study was performed to understand the molecular interactions of the synthesized compounds which revealed that the compounds perfectly docked into the active sites of the protein.
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