☆ 4.5 Article

Synthesis of potent antitumor and antiviral benzofuran derivatives

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 9, 页码 2420-2428

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.03.069

关键词

Furochromones; Benzofuran; Heterocyclic amines; Antitumor activity; Cytotoxicity; Antiviral activity; HIV and HIV-1 RT inhibitory activity; HCV NS3-4A protease inhibitor activity

类别

Chemistry, Medicinal Chemistry, Organic

资金

  1. USDA [BIO9-002-015]

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A new series of potent antitumor and antiviral benzofuran derivatives was synthesized by the reaction of the furochromone-6-carboxaldehydes 1 and 2 with different heterocyclic amines to yield the benzofuran-5-carbonyl derivatives 4-11. The synthesized compounds 1, 3-11 were tested against twelve different human cancer cell lines and all of the compounds were more potent than the comparative standards. The HIV inhibitory activity of the tested compounds 1, 3-11 showed that they have higher potency than Atevirdine. Moreover, compound 6 was significantly potent with wider therapeutic index. The HIV-1 RT inhibitory activity showed that compounds 10, 11, 3 and 4 were notably potent but with lower therapeutic index than Atevirdine. The HCV NS3-4A protease inhibitor activity of the tested compounds revealed that they have weaker potency and less therapeutic index than VX-950, although compounds 1, 4, 9 and 6, respectively exhibited significant activity. (c) 2009 Elsevier Ltd. All rights reserved.

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