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Anti-AIDS agents 73: Structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives.

Anti-AIDS agents 73: Structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives. Research Abstract Details 

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  • Anti-AIDS agents 73: Structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives. Abstract Text:

    keduo qianKeduo Qian,kyoko nakagawa-gotoKyoko Nakagawa-Goto,donglei yuDonglei Yu,susan l morris-natschkeSusan L Morris-Natschke,theodore j nitzTheodore J Nitz,nicole kilgoreNicole Kilgore,graham p allawayGraham P Allaway,kuo-hsiung leeKuo-Hsiung Lee,keduo qianKeduo Qian,kyoko nakagawa-gotoKyoko Nakagawa-Goto,donglei yuDonglei Yu,susan l morris-natschkeSusan L Morris-Natschke,theodore j nitzTheodore J Nitz,nicole kilgoreNicole Kilgore,graham p allawayGraham P Allaway,kuo-hsiung leeKuo-Hsiung Lee,

    3-O-3'(or 2')-Methylsuccinyl-betulinic acid (MSB) derivatives were separated by using recycle HPLC. The structures of four isomers were assigned by NMR and asymmetric synthesis. 3-O-3'S-Methylsuccinyl-betulinic acid (3'S-MSB, 4) exhibited potent anti-HIV activity with an EC(50) value of 0.0087muM and a TI value of 6.3x10(3), which is comparable to the data for bevirimat (DSB, PA-457), a current clinical trials drug that was also derived from betulinic acid. The anti-HIV potency of 4 was slightly better than that of AZT.

    Anti-AIDS agents 73: Structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives. Publishing Authors By Initials

    k qianK Qian,k nakagawa-gotoK Nakagawa-Goto,d yuD Yu,sl morris-natschkeSL Morris-Natschke,tj nitzTJ Nitz,n kilgoreN Kilgore,gp allawayGP Allaway,kh leeKH Lee,k qianK Qian,k nakagawa-gotoK Nakagawa-Goto,d yuD Yu,sl morris-natschkeSL Morris-Natschke,tj nitzTJ Nitz,n kilgoreN Kilgore,gp allawayGP Allaway,kh leeKH Lee,

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    Anti-AIDS agents 73: Structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives. Journal Published:

    PUBLICATION TYPE: Journal Article

    Journal: Bioorganic & medicinal chemistry letters

    VOLUME: 17

    Page Numbers: 6553-7

    Journal Abbreviation: Bioorg. Med. Chem. Lett.

    ISSN: 0960-894X

    DAY: 1

    MONTH: Dec

    YEAR: 2007

    Anti-AIDS agents 73: Structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives. Information

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    LANGUAGE: eng

    NlmUniqueID: 9107377

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    Grant and Affiliation Information for Anti-AIDS agents 73: Structure-activity relationship study and asymmetric synthesis of 3-O-monomethylsuccinyl-betulinic acid derivatives.

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

    Country: England

    England Research PublicationEngland Research Publication

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    MEDLINETA: Bioorg Med Chem Lett

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