Synthesis and anti-hepatitis C virus activity of novel ethyl 1H-indole-3-carboxylates in vitro |
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| Authors: | Grazia Sellitto Aurora Faruolo Paolo de Caprariis Sergio Altamura Giacomo Paonessa Gennaro Ciliberto |
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| Institution: | 1. Dipartimento di Scienze Farmaceutiche,Università di Salerno, Via Ponte Don Melillo, 84084 Fisciano, Italy;2. Istituto di Ricerche di Biologia Molecolare, Via Pontina km 30,600, Pomezia, Roma, Italy;3. Dipartimento di Medicina Sperimentale e Clinica ‘G. Salvatore’, Università degli Studi ‘Magna Graecia’ di Catanzaro, Italy |
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| Abstract: | A series of ethyl 1H-indole-3-carboxylates 9a1–6 and 9b1–2 were prepared and evaluated in Huh-7.5 cells. Most of the compounds exhibited anti-hepatitis C virus (HCV) activities at low concentration. The selectivity indices of inhibition on entry and replication of compounds 9a2 (>10; >16.7) and 9b1 (>6.25; >16.7) were higher than those of the other evaluated compounds, including the lead compound Arbidol (ARB, 6; 15). Moreover, the selective index of inhibition on entry of compound 9a3 (>6.25) was higher than that of ARB (6). Of these three initial hits, compound 9a2 was the most potent. |
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