Lee, JY Yoon, KJ Lee, YS 2024-01-21T07:43:20Z 2024-01-21T07:43:20Z 2021-09-03 2003-12-15 0960-894X https://pubs.kist.re.kr/handle/201004/137996 HIV integrase catalyzes the integration of HIV DNA copy into the host cell DNA, which is essential for the production of progeny viruses. L-Chicoric acid and dicaffeoylquinic acids, isolated from plants, are well known potent inhibitors of HIV integrase. The common structural features of these inhibitors are caffeic acid derivatives connected to tartaric acid or quinic acid through ester bonds. In the present study, we have synthesized and tested the inhibitory activities of a new type of HIV IN inhibitors, which has catechol groups in place of caffeoyl groups in the structure of L-chicoric acid. Upon substitution of catechol groups at succinic acid, pyrrol dicarboxylic acid, maleimide or maleic anhydride, the inhibitory activities (IC50 = 3.8-23.6 muM) were retained or remarkably increased when compared to parent compound L-chicoric acid (IC50 = 13.7 muM). (C) 2003 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD IMMUNODEFICIENCY-VIRUS TYPE-1 DICAFFEOYLTARTARIC ACIDS POTENT INHIBITORS REPLICATION ESTER Catechol-substituted L-chicoric acid analogues as HIV integrase inhibitors Article 10.1016/j.bmcl.2003.09.046 1 BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.13, no.24, pp.4331 - 4334 BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 13 24 4331 4334 scie scopus 000187010700015 2-s2.0-0344064865 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article IMMUNODEFICIENCY-VIRUS TYPE-1 DICAFFEOYLTARTARIC ACIDS POTENT INHIBITORS REPLICATION ESTER