2. Academic Validation
  3. Design, synthesis, and antitumor activity of bile acid-polyamine-nucleoside conjugates

Design, synthesis, and antitumor activity of bile acid-polyamine-nucleoside conjugates

  • Bioorg Med Chem Lett. 2007 Jun 1;17(11):2983-6. doi: 10.1016/j.bmcl.2007.03.067.
Dimao Wu 1,  Sanhao Ji,  Yan Wu,  Yong Ju,  Yufen Zhao
Affiliations

Affiliation

  • 1 Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Ministry of Education, Department of Chemistry, Tsinghua University, Beijing 100084, PR China.
PMID: 17416522 DOI: 10.1016/j.bmcl.2007.03.067
Abstract

A series of bile acid-polyamine amides conjugated with 3'-azido-3'-deoxythymidine (AZT) as potential antitumor prodrugs in the form of phosphoramidates were synthesized in good yields and their antitumor activities were assayed against two human Cancer cells in vitro: cervix Cancer HeLa cells and renal Cancer 7860 cells. The improved antitumor activity probably derived from the enhanced delivery efficiency of AZT due to bile acid-polyamine conjugates.

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