2. Academic Validation
  3. Synthesis and SAR of vinca alkaloid analogues

Synthesis and SAR of vinca alkaloid analogues

  • Bioorg Med Chem Lett. 2009 Feb 15;19(4):1245-9. doi: 10.1016/j.bmcl.2008.12.077.
Matthew E Voss 1,  Jeffery M Ralph,  Dejian Xie,  David D Manning,  Xinchao Chen,  Anthony J Frank,  Andrew J Leyhane,  Lei Liu,  Jason M Stevens,  Cheryl Budde,  Matthew D Surman,  Thomas Friedrich,  Denise Peace,  Ian L Scott,  Mark Wolf,  Randall Johnson
Affiliations

Affiliation

  • 1 Albany Molecular Research, Inc., 26 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA. [email protected]
PMID: 19147348 DOI: 10.1016/j.bmcl.2008.12.077
Abstract

Versatile intermediates 12'-iodovinblastine, 12'-iodovincristine and 11'-iodovinorelbine were utilized as substrates for transition metal based chemistry which led to the preparation of novel analogues of the vinca Alkaloids. The synthesis of key iodo intermediates, their transformation into final products, and the SAR based upon HeLa and MCF-7 cell toxicity assays is presented. Selected analogues 27 and 36 show promising Anticancer activity in the P388 murine leukemia model.

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