Natural products have served as inspirational scaffolds for the design and synthesis of novel antineoplastic agents. Here we present our preliminary efforts on the synthesis and biological evaluation of a new class of electrophilic steroids inspired by the naturally occurring taccalonolides. We demonstrate that these simplified analogs exhibit highly persistent antiproliferative properties similar to the taccalonolides and retain activity against resistant cancer cell lines that warrants further preclinical development.

中文翻译：

---

受他卡酮内酯启发的亲电子类固醇的合成和生物学评价

天然产物已成为设计和合成新型抗肿瘤药物的灵感支架。在这里，我们展示了受天然存在的他卡酮内酯启发，对一类新型亲电子类固醇的合成和生物学评估所做的初步努力。我们证明这些简化的类似物表现出与他卡酮内酯相似的高度持久的抗增殖特性，并保留了针对耐药癌细胞系的活性，这值得进一步的临床前开发。