Correlation of biologic data with physico-chemical properties among the vinca alkaloids and their congeners.
Correlation of biologic data with physico-chemical properties among the vinca alkaloids and their congeners.
复制标题
长春花生物碱及其同系物的生物数据与理化性质的相关性。
DOI：
10.1016/0006-2952(77)90108-3
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发表时间：
1977
影响因子：
5.8
通讯作者：
F. Hains
中科院分区：
文献类型：
--
作者：
R. Owellen;D. Donigian;C. Hartke;F. Hains
已证明，[3 H]长春碱与微管蛋白的结合被其他紫堇生物碱衍生物取代是一个竞争性过程，从而可以测定每种药物的缔合常数。LD 50数据和抗P-388活性与log P和log Ka之间存在相关性，相关方程为：log LD 50= 0.129（log P）2− 0.522 log P− 0.479 log Ka + 4.652 log P− 388= 0.222（log P）2− 1.059 log P− 0.520 log Ka + 5.366。长春新碱和去乙酰长春碱是该系列中活性最高的两种药物。后一种药物具有显著的生物活性是相当令人感兴趣的，因为已知它是人类代谢物。
Displacement of [3 H] vinblastine binding to tubulin by other Vinca alkaloid derivatives has been demonstrated to be a competitive process, allowing for determination of the association constant of each drug. Correlation of LD 50 data and anti-P-388 activity was found with log P and log K a, according to the equations: log LD 50= 0.129 (log P) 2− 0.522 log P− 0.479 log K a+ 4.652 log P− 388= 0.222 (log P) 2− 1.059 log P− 0.520 log K a+ 5.366. Vincristine and desacetylvinblastine were the two most active agents in this series. That the latter drug had significant biologic activity was of considerable interest, since it is known to be a human metabolite.