Celastrol and its derivatives have been reported for their potent anticancer activity. Among other celastrol analogues, novel carbamate derivatives were designed and synthesised, and their biological activity on the viability of human cancer cell lines was evaluated. Additionally, a preliminary structure–activity relationship study was conducted. Derivative 18 showed the highest activity on cancer cell viability, combined with the best selectivity between malignant cells and non-malignant fibroblasts. Preliminary mechanistic studies of its anti-tumour action indicated that compound 18 has an antiproliferative effect on SKOV-3 human ovarian cancer cells (IC₅₀ = 0.54 μM). The results also suggested that its potent anticancer activity is mediated by apoptosis, and that this process was mainly the result of the activation of the extrinsic apoptotic pathway. Moreover, our results demonstrated the potential of derivative 18 as a new agent for combinatorial drug therapy for ovarian cancer.

已经报道了Celastrol及其衍生物具有强大的抗癌活性。在其他Celastrol类似物中，设计并合成了新型氨基甲酸酯衍生物，并评估了它们对人类癌细胞系生存力的生物学活性。此外，进行了初步的结构-活性关系研究。衍生物18显示出对癌细胞生存力的最高活性，并与恶性细胞和非恶性成纤维细胞之间的最佳选择性结合。对其抗肿瘤作用的初步机理研究表明，化合物18对SKOV-3人卵巢癌细胞具有抗增殖作用（IC ₅₀ = 0.54μM）。该结果还表明其有效的抗癌活性是由细胞凋亡介导的，并且该过程主要是外在凋亡途径的激活的结果。此外，我们的结果证明了衍生物18作为卵巢癌组合药物治疗新药的潜力。