QUANTITATIVE-ANALYSIS OF ANTI-CYTOKININ ACTIVITY OF 4-SUBSTITUTED-2-METHYLTHIOPYRIDO[2,3-D]PYRIMIDINES

被引：25

作者：

IWAMURA, H ^{[1
]}

MURAKAMI, S ^{[1
]}

KOGA, JI ^{[1
]}

MATSUBARA, S ^{[1
]}

KOSHIMIZU, K ^{[1
]}

机构：

[1] KYOTO PREFECTURAL UNIV,APPL BIOL LAB,KYOTO 606,JAPAN

来源：

PHYTOCHEMISTRY | 1979年 / 18卷 / 08期

关键词：

Anticytokinins; pyrido[2,3-d]pyrimidines; structure-activity relationship; tobacco callus;

D O I：

10.1016/0031-9422(79)83004-6

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Ten 4-substituted-2-methylthiopyrido[2,3-d]pyrimidines were synthesized and tested for their cytokinin-antagonistic activity by the tobacco callus bioassay. This series of compounds constitutes the first example of anti-cytokinins which possess a fused 6-6 membered ring system. The treatment of Lineweaver and Burk, the method of classical enzyme kinetics, revealed competitive inhibition of cytokinin-induced tobacco callus growth. The variation of activity with the systematic transformation of 4-substituents was analysed quantitatively with physicochemical substituent parameters and regression analysis. The results indicated the predominant importance of substituent width for binding of the antagonists at the receptor site of cytokinins. © 1979.

引用

页码：1265 / 1268

页数：4

共 15 条

[1] CYTOKININS - DEVELOPMENT OF A POTENT ANTAGONIST [J].