Metabolism blocked classical folate analog inhibitors of dihydrofolate reductase-1: synthesis and biological evaluation of mobiletrex was written by Nair, M. Gopal;Fayard, Melanie L.;Lariccia, Joanna M.;Amato, Alaina E.;McGuire, John J.;Galivan, John H.;Kisliuk, Roy L.. And the article was included in Medicinal Chemistry Research in 1999.Electric Literature of C8H6N2O2 This article mentions the following:
A classical folate analog inhibitor of dihydrofolate reductase is described. This compound, 4′-methylene-5,8,10-trideazaaminopterin [Mobiletrex; M-Trex], is resistant to both polyglutamylation and aldehyde oxidase mediated 7-hydroxylation. Mobiletrex exhibited excellent inhibition of human dihydrofolate reductase and inhibited growth of a number of human tumor cells in culture. Unlike methotrexate, mobiletrex was not a substrate of either folylpolyglutamate synthetase or rabbit liver aldehyde oxidase. Mobiletrex caused total growth inhibition (TGI) of a number of human tumor cells at therapeutically relevant concentrations (â?1Ã10-6 M) which are potencies strikingly higher than those of methotrexate. In the experiment, the researchers used many compounds, for example, 5-Methyl-2-nitrobenzonitrile (cas: 64113-86-6Electric Literature of C8H6N2O2).
5-Methyl-2-nitrobenzonitrile (cas: 64113-86-6) belongs to nitriles. There has been no report on the microbial biosynthesis of nitriles and the physiological function of such enzymes, nor was it not even known whether aliphatic and aromatic nitriles are biological compounds or just petrochemicals. Alkyl nitriles are sufficiently acidic to undergo deprotonation of the C-H bond adjacent to the CN group.Strong bases are required, such as lithium diisopropylamide and butyl lithium. The product is referred to as a nitrile anion. Electric Literature of C8H6N2O2
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts