Syntheses and evaluation of novel fatty acid-second-generation taxoid conjugates as promising anticancer agents.
Basic Information
ID: ALA1138108
Journal: Bioorg Med Chem Lett
Title: Syntheses and evaluation of novel fatty acid-second-generation taxoid conjugates as promising anticancer agents.
Authors: Kuznetsova L, Chen J, Sun L, Wu X, Pepe A, Veith JM, Pera P, Bernacki RJ, Ojima I.
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.
CiteXplore: 16298526
DOI: 10.1016/j.bmcl.2005.10.089
Patent ID: ┄