Design, synthesis and SAR study of Fluorine-containing 3rd-generation taxoids.

ABSTRACT: It has been shown that the incorporation of fluorine or organofluorine groups into pharmaceutical and agricultural drugs often induces desirable pharmacological properties through unique protein-drug interactions involving fluorine. We have reported separately remarkable effects of the 2,2-difluorovinyl (DFV) group at the C3' position, as well as those of the CF₃O and CHF₂O groups at the 3-position of the C2-benzoyl moiety of the 2nd- and 3rd-generation taxoids on their potency and pharmacological properties. Thus, it was very natural for us to investigate the combination of these two modifications in the 3rd-generation taxoids and to find out whether these two modifications are cooperative at the binding site in the β-tubulin or not, as well as to see how these effec

SUBMITTER: Wang C 

PROVIDER: S-EPMC12352541 | biostudies-literature | 2022 Feb

REPOSITORIES: biostudies-literature