Anti-AIDS agents 66: syntheses and anti-HIV activity of phenolic and aza 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) derivatives.

Anti-AIDS agents 66: syntheses and anti-HIV activity of phenolic and aza 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) derivatives. Research Abstract Details 

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Anti-AIDS agents 66: syntheses and anti-HIV activity of phenolic and aza 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) derivatives. Abstract Text:

Madoka Suzuki,Donglei Yu,Susan L Morris-Natschke,Philip C Smith,Kuo-Hsiung Lee,Madoka Suzuki,Donglei Yu,Susan L Morris-Natschke,Philip C Smith,Kuo-Hsiung Lee,

New phenolic and aza 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) analogs were synthesized and assayed for inhibition of HIV-1 IIIB replication in H9 lymphocytes. Compound 16, 4-methyl-1'-aza-DCK (4-methyl-aza-DCK), was less lipophilic than 4-methyl-DCK, and retained sub-micromolar anti-HIV activity with EC(50) and TI values of 0.77 microM and >42, respectively. Moreover, it showed moderately improved metabolic stability. Introduction of phenolic hydroxyl groups to 4-methyl-DCK decreased lipophilicity significantly, but did not improve metabolic stability and also decreased activity.

Anti-AIDS agents 66: syntheses and anti-HIV activity of phenolic and aza 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) derivatives. Publishing Authors By Initials

M Suzuki,D Yu,SL Morris-Natschke,PC Smith,KH Lee,M Suzuki,D Yu,SL Morris-Natschke,PC Smith,KH Lee,

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Anti-AIDS agents 66: syntheses and anti-HIV activity of phenolic and aza 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) derivatives. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Bioorganic & medicinal chemistry

VOLUME: 15

Page Numbers: 6852-8

Journal Abbreviation: Bioorg. Med. Chem.

ISSN: 0968-0896

DAY: 13

MONTH: 12

YEAR: 2006

Anti-AIDS agents 66: syntheses and anti-HIV activity of phenolic and aza 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) derivatives. Information

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LANGUAGE: eng

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Grant and Affiliation Information for Anti-AIDS agents 66: syntheses and anti-HIV activity of phenolic and aza 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) derivatives.

AFFILIATION: Natural Products Research Laboratories, School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599-7360, USA.

Country: England

AGENCY: United States NIAID

GRANT: AI33066

ACRONYM: AI

MEDLINETA: Bioorg Med Chem

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