Rosowsky, Andre; Chen, Katherine K. N. published an article in 1974, the title of the article was Methotrexate analogs. 4. 7-Methyl derivatives of methotrexate and dichloromethotrexate. New synthesis and some biological studies.Safety of 2-Aminomalononitrile 4-methylbenzenesulfonate And the article contains the following content:
Conversion of methotrexate (I) [59-05-2] and 3′,5′-dichloromethotrexate (II) [528-74-5] to their 7-methyl analogs III [35190-25-1] and IV [53729-18-3], resp., to prevent metabolism in vivo to the inactive 7-hydroxy derivatives resulted in marked loss of antileukemic activity in mice and in vitro and loss of inhibitory potency against purified dihydrofolate reductase [9002-03-3] from Lactobacillus casei and L1210-FR8 tumor. The lack of antitumor activity presumably resulted from impaired enzyme binding. III was prepared from 2-amino-5-chloromethyl-3-cyano-6-methylpyrazine 1-oxide [53661-20-4] and diethyl N-(p-N-methylaminobenzoyl)glutamate [2378-95-2] by the method of E. C. Taylor, et al. (1973). The experimental process involved the reaction of 2-Aminomalononitrile 4-methylbenzenesulfonate(cas: 5098-14-6).Safety of 2-Aminomalononitrile 4-methylbenzenesulfonate
The Article related to methotrexate analog leukemia, dihydrofolate reductase methotrexate analog, Pharmacodynamics: Structure-Activity and other aspects.Safety of 2-Aminomalononitrile 4-methylbenzenesulfonate
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