Structure and absolute stereochemistry of HIV-1 integrase inhibitor integric acid. A novel eremophilane sesquiterpenoid produced by a Xylaria sp.

Authors
Singh, SB Zink, D Polishook, J Valentino, D Shafiee, A Silverman, K Felock, P Teran, A Vilella, D Hazuda, DJ Lingham, RB
Citation
Sb. Singh et al., Structure and absolute stereochemistry of HIV-1 integrase inhibitor integric acid. A novel eremophilane sesquiterpenoid produced by a Xylaria sp., TETRAHEDR L, 40(50), 1999, pp. 8775-8779
Citations number
8
Categorie Soggetti
Chemistry & Analysis","Organic Chemistry/Polymer Science
Journal title
TETRAHEDRON LETTERS
ISSN journal
00404039 → ACNP
Volume
40
Issue
50
Year of publication
1999
Pages
8775 - 8779
Database
ISI
SICI code
0040-4039(199912)40:50<8775:SAASOH>2.0.ZU;2-R
Abstract
HIV-1 integrase is critical for viral replication and is absent in the host , and therefore is a potential target for the development of non-toxic anti viral therapy. From the screening of natural product libraries we have disc overed integric acid, a novel eremophilane sesquiterpenoid, from a Xylaria sp. It inhibited 3'-end processing, strand transfer and disintegration reac tions catalyzed by HIV-1 integrase with IC50 values of 3-10 mu M. The isola tion, structure elucidation, relative, and absolute stereochemistry of inte gric acid are described. (C) 1999 Elsevier Science Ltd. All rights reserved .