2. Academic Validation
  3. Synthesis and cytotoxic evaluation of novel ester-triazole-linked triterpenoid-AZT conjugates

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

  • Bioorg Med Chem Lett. 2014 Nov 15;24(22):5190-4. doi: 10.1016/j.bmcl.2014.09.079.
Tuyet Anh Dang Thi 1,  Nguyen Thi Kim Tuyet 1,  Chinh Pham The 1,  Ha Thanh Nguyen 1,  Cham Ba Thi 1,  Tien Doan Duy 1,  Matthias D'hooghe 2,  Tuyen Van Nguyen 3
Affiliations

Affiliations

  • 1 Institute of Chemistry, Vietnam Academy of Science and Technology, 18-Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam.
  • 2 SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, Belgium.
  • 3 Institute of Chemistry, Vietnam Academy of Science and Technology, 18-Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam. Electronic address: ngvtuyen@hotmail.com.
PMID: 25442310 DOI: 10.1016/j.bmcl.2014.09.079
Abstract

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.

Keywords

AZT; Cytotoxic agents; Hybrids; Triterpenoids.

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