Biological Evaluation of 5-Substituted Pyrimidine Derivatives as Inhibitors of Brassinosteroid Biosynthesis
Biological Evaluation of 5-Substituted Pyrimidine Derivatives as Inhibitors of Brassinosteroid Biosynthesis
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5-取代嘧啶衍生物作为油菜素类固醇生物合成抑制剂的生物学评价
DOI：
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发表时间：
2001
期刊：
影响因子：
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通讯作者：
N. Murofushi
中科院分区：
文献类型：
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作者：
Jing;T. Asami;S. Yoshida;N. Murofushi
合成了一系列5-取代嘧啶衍生物，并测试了它们抑制油菜素内酯生物合成的能力。用水芹茎伸长法评价了化合物的生物活性。在所合成的化合物中，α-（4-氯苯基）-α-苯基-5-嘧啶甲醇（DPPM 4）在光照条件下对水芹茎伸长有明显的抑制作用。这种抑制作用可被10 nM油菜素钠逆转，但不能被1 μM GA 3逆转。DPPM 4也影响拟南芥在黑暗中的生长。DPPM 4处理的拟南芥在黑暗中具有类似于油菜素内酯缺陷突变体的表型，具有短的下胚轴和开放的子叶。这些生物学变化可通过10 nM油菜素内酯的共同应用而恢复，但不能通过1 μM GA 3，表明DPPM 4的主要作用位点是油菜素类固醇生物合成途径。
A series of 5-substituted pyrimidine derivatives was synthesized, and their ability to inhibit brassinosteroid biosynthesis was tested. The biological activity of these compounds was evaluated by the cress stem elongation method. Among the synthesized compounds, α-(4-chlorophenyl)-α-phenyl-5-pyrimidinemethanol (DPPM 4) exhibited potent inhibitory activity for retarding cress stem elongation in the light. This inhibition was reversed by the application of 10 nM brassinolide, but not by 1 μM GA3. DPPM 4 also affected Arabidopsis growth in the dark. DPPM 4-treated Arabidopsis had phenotypes like those of brassinosteroid-deficient mutants, with short hypocotyls and open cotyledons, in the dark. These biological changes were restored by the co-application of 10 nM brassinolide, but not by 1 μM GA3, suggesting that the primary site of action of DPPM 4 was the brassinosteroid biosynthetic pathway.