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Metal-dependent inhibition of HIV-1 integrase.

Abstract：

:Human immunodeficiency virus type 1 integrase (HIV-1 IN) is an essential enzyme for effective viral replication. Therefore, IN inhibitors are being sought for chemotherapy against AIDS. We had previously identified a series of salicylhydrazides as potent inhibitors of IN in vitro (Neamati, N.; et al. J. Med. Chem. 1998, 41, 3202-3209.). Herein, we report the design, synthesis, and antiviral activity of three novel mercaptosalicylhydrazide (MSH) derivatives. MSHs were effective against the IN catalytic core domain and inhibited IN binding to HIV LTR DNA. They also inhibited catalytic activities of IN in IN-DNA preassembled complexes. Site-directed mutagenesis and molecular modeling studies suggest that MSHs bind to cysteine 65 and chelate Mg(2+) at the active site of HIV-1 IN. Contrary to salicylhydrazides, the MSHs are 300-fold less cytotoxic and exhibit antiviral activity. They are also active in Mg(2+)-based assays, while IN inhibition by salicylhydrazides is strictly Mn(2+)-dependent. Additionally, in target and cell-based assays, the MSHs have no detectable effect on other retroviral targets, including reverse transcriptase, protease, and virus attachment, and exhibit no detectable activity against human topoisomerases I and II at concentrations that effectively inhibit IN. These data suggest that MSHs are selective inhibitors of HIV-1 IN and may serve as leads for antiviral therapeutics.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Neamati N,Lin Z,Karki RG,Orr A,Cowansage K,Strumberg D,Pais GC,Voigt JH,Nicklaus MC,Winslow HE,Zhao H,Turpin JA,Yi J,Skalka AM,Burke TR Jr,Pommier Y

doi

10.1021/jm0201417

keywords:

subject

Has Abstract

pub_date

2002-12-19 00:00:00

pages

5661-70

issue

26

eissn

0022-2623

issn

1520-4804

pii

jm0201417

journal_volume

45

pub_type

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