STRUCTURE-ACTIVITY-RELATIONSHIPS OF BENZIMIDAZOLE CARBAMATES AS INHIBITORS OF MAMMALIAN TUBULIN, INVITRO
STRUCTURE-ACTIVITY-RELATIONSHIPS OF BENZIMIDAZOLE CARBAMATES AS INHIBITORS OF MAMMALIAN TUBULIN, INVITRO
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DOI：
10.1016/0006-2952(85)90611-2
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发表时间：
1985-01-01
影响因子：
5.8
通讯作者：
WATSON, TR
中科院分区：
文献类型：
--
作者：
LACEY, E;WATSON, TR
研究了32-甲基(5(6)-取代苯并咪唑-2基)氨基甲酸酯作为微管蛋白聚合速率抑制剂的构效关系。5(或6)位取代基的大小或某些共线的物理化学特性对效力有深远的影响。支化的存在以及与苯并咪唑环(α位置)相邻的5(6)-取代基极性的相应增加或不相应地增加，导致活性丧失。定量模型反映的整个位置的性质可能与5(或6)-取代基的疏水性或摩尔体积有关。
The structure-activity relationships of 32 methyl (5(6)-substituted benzimidazol-2yl) carbamates as inhibitors of the rate of polymerisation of tubulin were investigated. The size or some colinear physico-chemical characteristic of the substituent in the 5 (or 6)-position has a profound effect on potency. The presence of branching, with or without a commensurate increase in the polarity of the 5(6)-substituent adjacent to the benzimidazole ring (.alpha.-position), resulted in a loss of activity. The nature of the overall site, as reflected by the quantitative models, could relate to either the hydrophobicity or molar volume of the 5 (or 6)-substituents.