Etodolac Thiosemicarbazides:A novel class of hepatitis C virus NS5B polymerase inhibitors

Anti-cancer and anti-hepatitis C virus NS5B polymerase activity of etodolac 1,2,4-triazoles

“…These etodolac derivatives were designed and prepared as described previously in our studies [14][15][16] .…”

“…The five-membered heterocyclic ring of the triazoles has served as an important scaffold for many bioactive compounds, some of which have emerged as effective and non-toxic antitumor drugs derivatives, on the other hand, have been documented as potent in vitro anti-HCV NS5B polymerase inhibitor 12,13 . We recently reported on the synthesis of etodolac thiosemicarbazides and identified their anti-HCV NS5B polymerase activity 14 .…”

“…The reaction of corresponding hydrazide 2 with respective alkyl/aryl isothiocyanates yielded etodolac thiosemicarbazides (3a-h) 14,16 . In present study, smooth cyclization of etodolac thiosemicarbazides under alkaline condi- The refluxing of etodolac thiosemicarbazides in aqueous NaOH transformed into the target compounds (4a-h) was indicated in the IR spectra by appearance of a single absorption for NH in the region 3160-3349 cm À1 and disapperance of a comparatively strong band in the region 1674-1688 cm À1 for the carbonyl of hydrazides, indicated the formation of triazoles.…”

Design, synthesis, and in vitro and in vivo anticancer activity studies of new (S)-Naproxen thiosemicarbazide/1,2,4-triazole derivatives

“…They have various pharmacological activities, especially anticancer activity. [25][26][27][28][29][30][31][32][33][34][35] The 1,2,4-triazole ring is a five-membered heterocyclic ring that includes two carbon and three nitrogen atoms. The 1,2,4-triazole ring is synthesized by heating thiosemicarbazides in a basic medium.…”

Synthesis and Anticancer Activity of Tolmetin Thiosemicarbazides

“…Duffy and co-workers evaluated that tolmetin and other (NSAID)s have effects on increasing the cytotoxic activity of the anti-cancer drugs (3). Thiosemicarbazides, which are intermediate products of the synthesis for bioactive heterocyclic compounds, have taken attention of the researchers because of their clinical use and diverse biological activities (4)(5)(6)(7)(8)(9)(10)(11)(12)(13)(14) (Fig 1). In this work, we synthesized novel ten tolmetin thiosemicarbazide derivatives (4a-j) and investigated their anticancer activity against cancer cell lines.…”