43074-77-7Relevant academic research and scientific papers
Synthesis, crystal structure and biological properties of a new series of lipophilic s-triazines, dihydrofolate reductase inhibitors
Tsitsa,Antoniadou-Vyza,Hamodrakas,Eliopoulos,Tsantili-Kakoulidou,Lada-Hytiroglou,Roussakis,Chinou,Hempel,Camerman,Ottensmeyer,Vanden Berghe
, p. 149 - 158 (1993)
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 to DHFR were determined experimentally. Compounds mono-substituted at the nitrogen of the amine group appear to be slightly better inhibitors. Weak activity was also enhanced by the presence of a methylene bridge between the adamantyl group and the s-triazine ring. The majority of the compounds was shown to have weak activity against P388 and KB cell lines in vitro; some compounds showed weak anti-bacterial activity and no anti-viral activity was detected.
