2. Academic Validation
  3. Syntheses and evaluation of novel fatty acid-second-generation taxoid conjugates as promising anticancer agents

Syntheses and evaluation of novel fatty acid-second-generation taxoid conjugates as promising anticancer agents

  • Bioorg Med Chem Lett. 2006 Feb 15;16(4):974-7. doi: 10.1016/j.bmcl.2005.10.089.
Larissa Kuznetsova 1,  Jin Chen,  Liang Sun,  Xinyuan Wu,  Antonella Pepe,  Jean M Veith,  Paula Pera,  Ralph J Bernacki,  Iwao Ojima
Affiliations

Affiliation

  • 1 Department of Chemistry, State University of New York at Stony Brook, Stony Brook, NY 11794-3400, USA.
PMID: 16298526 DOI: 10.1016/j.bmcl.2005.10.089
Abstract

Polyunsaturated fatty acids such as docosahexaenoic acid (DHA), linolenic acid, and linoleic acid were linked to the C-2' position of the second-generation taxoids that could overcome MDR caused by overexpressed ABC transporters. The new conjugates, tested in vivo, exhibited strong activity against drug-resistant colon Cancer and drug-sensitive ovarian Cancer xenografts in mice. Two of the new conjugates, DHA-SB-T-1214 and DHA-SB-T-1213, were found to achieve the total regression of drug-resistant and drug-sensitive tumors, respectively, in the animal models with substantially reduced systemic toxicity.

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