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Paper | Regular issue | Vol 45, No. 2, 1997, pp.241-253
Published online, 1st January, 1970
DOI: 10.3987/COM-96-7608
Synthesis of Some Conformationally-constrained Glutamate Mimics of N-{5-[2-Amino-3,4-dihydro-4-oxo-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidine-6-yl)ethyl]thien-2-ylcarbonyl]-L-glutamic Acid (LY254155)

Edward C. Taylor* and Baihua Hu

*Department of Chemistry, Princeton University, Princeton, New Jersey 08544, U.S.A.

Abstract

Several new analogues of the active antitumor agent N-{5-[2-(2-amino-3,4-dihydro-4-oxo-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)ethyl]thien-2-ylcarbonyl}-L-glutamic acid (LY254155) have been prepared in which the glutamate moiety has been replaced with conformationally-constrained azetidine and cyclopropane mimics. None of these new analogues exhibited significant cell growth inhibitory activity.