The natural product (+)-grandifloracin is a potent "anti-austerity" agent, able to suppress the ability of various pancreatic cancer cell lines to tolerate conditions of nutrient deprivation. Such anti-austerity agents represent a promising approach to cancer chemotherapy. Here we report the synthesis and biological evaluation of racemic analogues of grandifloracin bearing diverse sidechains, of which two show enhanced potency in comparison with the natural product. Additionally, several unexpected by-products containing modifications of the grandifloracin core were isolated, identified and similarly evaluated for biological activity.

中文翻译：

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Grandifloracin的侧链多样化允许鉴定具有增强的针对人PANC-1胰腺癌细胞的抗紧缩活性的类似物。

天然产物（+）-大花青素是有效的“抗紧缩”剂，能够抑制各种胰腺癌细胞系耐受营养剥夺条件的能力。此类抗紧缩剂代表了癌症化学疗法的有前途的方法。在这里，我们报告了带有多种侧链的大花甙的外消旋类似物的合成和生物学评估，其中两个与天然产物相比显示出增强的效价。另外，分离，鉴定并相似地评估了含有大花环素核心修饰的几种意想不到的副产物的生物学活性。