Rimoldi J M, Kingston D G, Chaudhary A G, Samaranayake G, Grover S, Hamel E
Department of Chemistry, Virginia Polytechnic Institute and State University, Blacksburg 24061-0212.
J Nat Prod. 1993 Aug;56(8):1313-30. doi: 10.1021/np50098a016.
The 7-substituted taxol analogues 7, 19, 27, and 32 have been prepared as potential photoaffinity-labeled derivatives for studies of the nature of the binding site of taxol on polymerized tubulin. The analogue 32 has been prepared in both deuterium- and tritium-labeled versions. Tubulin-assembly studies were carried out with these compounds, and it was found that they showed some but not all of the properties of taxol. We conclude that these specific taxol analogues labeled at the 7 position are not ideal derivatives for photoaffinity labeling studies.
已制备出7-取代紫杉醇类似物7、19、27和32，作为潜在的光亲和标记衍生物，用于研究紫杉醇在聚合微管蛋白上结合位点的性质。类似物32已制备出氘标记和氚标记两种版本。用这些化合物进行了微管蛋白组装研究，发现它们表现出紫杉醇的一些但并非全部性质。我们得出结论，这些在7位标记的特定紫杉醇类似物并非光亲和标记研究的理想衍生物。
