Hwang, DJ Kim, SN Choi, JH Lee, YS 2024-01-21T12:14:17Z 2024-01-21T12:14:17Z 2021-09-05 2001-06 0968-0896 https://pubs.kist.re.kr/handle/201004/140456 Human immunodeficiency virus (HIV) integrase (IN) catalyzes the integration of HIV DNA copy into the host cell DNA. Such integration is essential for the production of progeny viruses, and therefore therapeutic agents that can inhibit this process should be effective anti-HIV agents. We have previously reported the inhibitory activity of dicaffeoylglucosides against HIV IN. In the present study, we have synthesized and tested dicaffeoyl or digalloyl compounds joined through a five-membered heterocyclic ring as HIV IN inhibitors to explore the SARs of this family of compounds. The starting heterocyclic diols were prepared from L-tartaric acid, diethyl L-tartarate or D-(+)-ribonic gamma -lactone. We found that the HIV IN inhibitory activities of dicaffeoyl derivatives were comparable to that of L-chicoric acid (IC50 = 24.9 muM). On the other hand, digalloyl derivatives were more potent than L-chicoric acid with IC50 Values of 4.7-15.6 muM. (C) 2001 Elsevier Science Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD IMMUNODEFICIENCY-VIRUS TYPE-1 POTENT INHIBITORS REPLICATION ANALOGS ACIDS Dicaffeoyl- or digalloyl pyrrolidine and furan derivatives as HIV integrase inhibitors Article 10.1016/S0968-0896(01)00013-X 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.9, no.6, pp.1429 - 1437 BIOORGANIC & MEDICINAL CHEMISTRY 9 6 1429 1437 scie scopus 000169404600005 2-s2.0-0034930519 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article IMMUNODEFICIENCY-VIRUS TYPE-1 POTENT INHIBITORS REPLICATION ANALOGS ACIDS HIV