
Tetrahedron p. 1631 - 1638 (1999)
Update date:2022-08-02
Topics:
Taylor, Edward C.
Chaudhuri, Rajendra P.
Watson, Samuel E.
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.
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