ChemInform Abstract: Synthesis and anti-HIV Activity of New Homo Acyclic Nucleosides. 1-(Pent-4-enyl)quinoxalin-2-ones and 2-(Pent-4-enyloxy)quinoxalines

Autor:	Ibrahim A. I. Ali, Iman A. Al-Masoudi, H. Gh. Hassan, Najim A. Al-Masoudi
Rok vydání:	2008
Předmět:	Anti hiv activity chemistry.chemical_compound Quinoxaline Chemistry Stereochemistry General Medicine
Zdroj:	ChemInform. 39
ISSN:	1522-2667 0931-7597
DOI:	10.1002/chin.200815161
Popis:	A series of acyclonucleosides 6,7-disubstituted 1-(pent-4-enyl)quinoxalin-2-one derivatives and the O-analogs were synthesized by a one-step condensation of the corresponding quinoxaline bases with 5-bromo-1-pentene.The acyclonucleosides prepared were assayed against HIV-1 and HIV-2 in MT-4 cells. 6,7-Dimethyl-2-(pent-4-enyloxy)quinoxaline showed inhibition of HIV-1 with EC50 value of 0.22 ± 0.08 µg/ml and a therapeutic index of 13. This means that it was cytotoxic to MT-4 cells at CC50 of 2.6 ± 0.1 µg/ml.
Databáze:	OpenAIRE
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