146307-39-3Relevant academic research and scientific papers
Design and synthesis of releasable folate-drug conjugates using a novel heterobifunctional disulfide-containing linker
Satyam, Apparao
supporting information; experimental part, p. 3196 - 3199 (2009/04/11)
Cellular uptake of vitamin folic acid occurs via folate-receptor mediated endocytosis. Many types of cancer cells express high levels of folate receptors as they need continuous supply of this vitamin for their proliferation. With an objective to use foli
Synthesis and evaluation of Taxol-folic acid conjugates as targeted antineoplastics
Lee, Jae Wook,Lu, June Y.,Low,Fuchs
, p. 2397 - 2414 (2007/10/03)
A series of Taxol derivatives tethered at C2′ and C-7 to glutamate and folate have been synthesized for evaluation as prodrugs which release Taxol via hydrolytic lability of their α-alkoxy and α-amino esters. The half-time for hydrolysis of these materials was determined in pH 7 and pH 5 buffer. The in vitro cytotoxicity has been assessed in cell culture against A-549 lung cancer, MCF-7 breast cancer, and HT-29 colon cancer. Selected agents were further screened for folate binding and competitive binding with free folic acid. One agent (54), further evaluated in animal studies was found to increase the lifespan in mice, but was less effective than Taxol itself.
