Synthesis, crystal structure and biological properties of a new series of lipophilic s-triazines, dihydrofolate reductase inhibitors

…, A Tsantili-Kakoulidou, E Lada-Hytiroglou…

Index: Tsitsa; Antoniadou-Vyza; Hamodrakas; Eliopoulos; Tsantili-Kakoulidou; Lada-Hytiroglou; Roussakis; Chinou; Hempel; Camerman; Ottensmeyer; Vanden Berghe European Journal of Medicinal Chemistry, 1993 , vol. 28, # 2 p. 149 - 158

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Citation Number: 22

Abstract

Abstract A number of adamantyl-group-bearing diamino-s-triazines were synthesized as potential dihydrofolate reductase (DHFR) inhibitors and their pharmacological properties were tested. The crystal structures of certain compounds were determined by X-ray crystallography. With the aid of computer graphics, model structures of the L1210 mouse DHFR-ligand ternary complex were constructed. The binding affinities of the compounds ...