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Paper | Regular issue | Vol 45, No. 11, 1997, pp.2229-2237
Published online, 1st January, 1970
DOI: 10.3987/COM-97-7963
Synthesis of a Pyrido[2,3-d]pyrimidine Analogue of the Multitargeted Antifolate LY231514

Edward C. Taylor* and Koo Lee

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

Abstract

Synthesis of pyrido[2,3-d]pyrimidines (9) and (21), ring-expanded analogues of the antitumor agent LY231514 (7), and its 4-amino analog, respectively, are described. Preliminary in vitro cell culture evaluation has shown that expansion of the pyrrole ring of the latter two pyrrolo[2,3-d]pyrimidines through introduction of a carbonyl group between positions 6 and 7 results in complete loss of cell growth inhibitory activity.