Equisetin and a novel opposite stereochemical homolog phomasetin, two fungal metabolites as inhibitors of HIV-1 integrase

Autor:	Sheo B. Singh, Anne W. Dombrowski, Deborah L. Zink, Daria J. Hazuda, Michael A. Goetz, Jon D. Polishook
Rok vydání:	1998
Předmět:	chemistry.chemical_classification biology Stereochemistry Organic Chemistry Phomasetin biology.organism_classification Biochemistry In vitro law.invention Integrase Enzyme chemistry law Drug Discovery Recombinant DNA biology.protein Phoma Hiv 1 integrase Ic50 values
Zdroj:	Tetrahedron Letters. 39:2243-2246
ISSN:	0040-4039
DOI:	10.1016/s0040-4039(98)00269-x
Popis:	Integration is an essential step in HIV replication and is catalyzed by an enzyme called integrase. We have isolated equisetin (1a), and a novel opposite stereochemical homolog, phomasetin (2a), from Fusarium heterosporum and a Phoma sp. respectively. They inhibit the invitro recombinant integrase enzyme with IC50 values of 7–20 μM. Unlike known inhibitors, these compounds also inhibit the integration reactions catalyzed by preintegration complexes isolated from HIV-1 infected cells.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::f9b9924f7a333d118062ea292c6c2c16 https://doi.org/10.1016/s0040-4039(98)00269-x Zobrazit plný text záznamu Full Text from ScienceDirect