epothilone类构效关系及生物合成、转化的研究进展

epothilone类化合物大多数具有明显的抗肿瘤作用，并且在来源、合成方法、亲水性、抗肿瘤活性和抗肿瘤谱等方面均优于紫杉醇类药物，是一类新型抗肿瘤药物。近年来，对大量epothilone及其类似物进行了生物活性测定及药效学试验，并借助计算机分析，进行三维定量构效关系研究。在大规模发酵条件下，主要得到epothilone A和B以及C，D，E等少量成分，其中epothilone B和D被普遍认为是目前比较有效的抑瘤剂。这些化合物之间存在着某些生物转化关系，有可能会产生新的活性物质。本文主要叙述了该类化合物的构效关系、生物合成及相关转化的研究进展。

Advances in research on the structure-activity relationship,biosynthesis and biotransformation of epothilones

Most epothilones exhibit superior antitumor activity against human tumor cell lines to paclitaxel in resource, methods of synthesis, water solubility, and antitumor spectrum. Recently, bioactivity determination and pharmacodynamic experiment have been done, as well as 3D quantitative structure-activity relationship study. Epothilone A, B and C, D , E are obtained from large scale fermentation , and epothilone B, D are presumed as the most active antitumor agents. There are biotransformation relationships between these compounds which may generate new active substances. This article presents a review of structure-activity relationship , biosynthesis and biotransformation of these compounds.