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前文报导了某些邻苯二甲酰谷氨酰胺衍生物有抑制谷氨酰胺酶的作用,其中以邻笨二甲酰谷氨酰间三氟甲基苯胺作用最强。为了寻找抗肿瘤药物和了解化学结构与生物活性间的关系,又合成了邻苯二甲酰和取代邻苯二甲酰的谷氨酰取代苯胺及萘胺衍生物;以及开环的邻位羧基或氨甲酰基苯甲酰胺衍生物和间位及对位羧基取代的苯磺酰谷氨酰胺衍生物共24个化合物。此外还合成了α-N-琥珀酰谷氨酰胺及谷氨酰β-萘胺。以上化合物均进行了对酶抑制作用的研究,初步指出结构与抗谷氨酰胺酶活性之间的关系。
The foregoing reports that certain phthalyl glutamine derivatives have the effect of inhibiting glutaminase, of which the most potent is o-benzenedaronyl glutamyltrimethyl aniline. In order to find antitumor drugs and to understand the relationship between chemical structure and biological activity, and the synthesis of phthaloyl and substituted phthaloyl-substituted glutamyl aniline and naphthylamine derivatives; and ring-opened ortho-carboxyl Or a total of 24 compounds of carbamoyl benzamide derivatives and benzenesulfonyl glutamine derivatives substituted by meta and para carboxyl groups. In addition, α-N-succinyl glutamine and glutamine β-naphthylamine were also synthesized. The above compounds were studied on the enzyme inhibition, initially pointed out the relationship between structure and anti-glutaminase activity.