Tetrahedron

Potential silicon-containing antifolates

EC Taylor, RP Chaudhuri, SE Watson

Index: Taylor, Edward C.; Chaudhuri, Rajendra P.; Watson, Samuel E. Tetrahedron, 1999 , vol. 55, # 6 p. 1631 - 1638

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Citation Number: 9

Abstract

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 ...