(57)< Abstract > Through the reduction die folic acid receptor, it is transported to the tumor cell, enzyme dihydro folic acid reductase being unknown so far, being inactive be renewed, it offers the conventional folic acid salt similar thing inhibiter. These chemical compounds by comparison with metotorekiseto and canonical medicine theophylline, show the anti- asthmatic response which is superior in the rabbit. The chemical compound 4 amino 4 deoxy 5,8,10 torideaza 4 `- methylene glutamic acid of title (1) showed remarkable anti- tumor operation. As for chemical compound (1), the occasion where entire breeding obstruction (TGI) of the culture human tumor cell is caused many, activity 1,000 - 10,000 times was stronger than metotorekiseto. Unlike metotorekiseto, (1) TGI is inside the range of the concentration which has relation in remedy. The tumor cell which in the dot, porigurutamiru conversion deficiency does not show sensitivity in metotorekiseto 3 - 4 times showed sensitivity indirectly strongly in chemical compound (1). (1) when with huoriporigurutaminshintetaze inkiyubeshiyon doing, was inactive completely. When (1) treating with the aldehyde oxydase formulation, oxidation activity did not appear. Chemical compound 1 does not receive the hydrolysis disconnection of the gurutameto part with karubokishipepuchidaze of Pseudomonas genus fungus (Pseudononad sp.) origin completely. Be renewed the inactive conventional folic acid competition medicine this kind of biochemistry and pharmacology property, high target enzyme specificity and virulence is shown low being new, establish clinical utilization Characteristic and excellence Characteristic as a new anti- inflammation medicine and an anti- tumor medicine. < Conversion 1 >還元型葉酸受容体を介して腫瘍細胞に移送される、酵素ジヒドロ葉酸レダクターゼのこれまで未知で、代謝的に不活性で古典的な葉酸塩類似物阻害剤を提供する。これらの化合物は、メトトレキセートおよび標準的な薬剤テオフィリンと比較して、ウサギにおいて優れた抗喘息応答を示す。表題の化合物4-アミノ-4-デオキシ-5,8,10-トリデアザ-4‘-メチレングルタミン酸(1)は顕著な抗腫瘍作用を示した。化合物(1)は、数多くの培養ヒト腫瘍細胞の総増殖阻止(TGI)を生じる際に、メトトレキセートより活性が1
