Potential silicon-containing antifolates

Article abstract of DOI:10.1016/S0040-4020(98)01207-1

Novel silicon-containing folate derivatives were synthesized as potential inhibitors of folate-dependent enzymes in an attempt to develop more effective antitumor agents. A dimethylsilyl moiety was inserted into the sidechain of two known antifolates with the aim of improving passive transport properties and sidechain conformational flexibility. An efficient, convergent palladium-catalyzed coupling methodology was used to link known heterocycles to novel, highly functionalized vinyl and ethynyl silanes.