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紫杉醇是从短叶紫杉（Taxusbrevufolia）树中分离到的一个产物，它是强效微管稳定剂，临床用于治疗卵巢癌。但它的水不溶性（＜0．004mg·mL-1）影响了临床应用。本文报道了紫杉醇前药的设计、合成和生物活性，以改善其药理性质。要求设计的前药水溶性增强，在碱性或生理条件下可释放出紫杉醇。实验结果表明，这些前药在pH≤7时稳定，在碱性介质中可释放紫杉醇，并对微管有稳定作用。人血浆可以催化紫杉醇的释放，因而紫杉醇前药作为抗癌药比其母体化合物有更大的应用潜力。
Paclitaxel, a product isolated from the Taxus brevisfolia tree, is a potent microtubule stabilizer that is clinically used to treat ovarian cancer. However, its water insolubility (<0.004 mg · mL-1) has impacted the clinical application. This article reports the design, synthesis and bioactivity of paclitaxel prodrugs to improve their pharmacological properties. Requires prodrugs designed to enhance water solubility, in alkaline or physiological conditions can release paclitaxel. Experimental results show that these prodrugs are stable at pH <7, release paclitaxel in alkaline medium, and stabilize microtubules. Human plasma can catalyze the release of paclitaxel, and thus paclitaxel prodrugs have greater potential as anticancer drugs than their parent compounds.