Synthesis and cytotoxic evaluation of novel ester-triazole-linked triterpenoid-AZT conjugates

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:24

Article

Tuyet Anh Dang Thi¹  Nguyen Thi Kim Tuyet¹  Chinh Pham The¹  Ha Thanh Nguyen¹  Cham Ba Thi¹  Tien Doan Duy¹  D'hooghe, Matthias²  Tuyen Van Nguyen¹ 

[1] Vietnam Acad Sci & Technol, Inst Chem, Hanoi, Vietnam

[2] Univ Ghent, Fac Biosci Engn, Dept Sustainable Organ Chem & Technol, SynBioC Res Grp, B-9000 Ghent, Belgium

关键词: Triterpenoids;    AZT;    Hybrids;    Cytotoxic agents;   

DOI  :  10.1016/j.bmcl.2014.09.079

来源: Elsevier

【 摘 要 】

Betulinic acid and analogous naturally occurring triterpenoid acids were transformed into the corresponding propargyl esters and subsequently deployed as substrates for a click chemistry-mediated coupling with azidothymidine (AZT) en route to novel 1,2,3-triazole-tethered triterpenoid-AZT conjugates. Twelve new hybrids were thus prepared and assessed in terms of their cytotoxic activity, revealing an interesting anticancer activity of five triterpenoid-AZT hybrids on KB and Hep-G2 tumor cell lines. (C) 2014 Elsevier Ltd. All rights reserved.

【 授权许可】

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