A series of novel triptolide/furoxans hybrids were designed and synthesized as analogues of triptolide, which is a naturally derived compound isolated from the thunder god vine (Tripterygium wilfordii Hook. F). Some of these synthesized compounds exhibited antiproliferative activities in the nanomolar range. Among them, compound 33 exhibited both good antiproliferative activity and NO-releasing ability and the acute toxicity of compound 33 decreased more than 160 times (LD50 = 160.9 mg/kg) than triptolide. Moreover, compound 33 significantly inhibited the growth of melanoma at a low dose (0.3 mg/kg) and showed strong anti-inflammatory activity in vitro and in vivo. These results indicate that compound 33 could be a promising candidate for further study.

中文翻译：

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雷公藤甲素的新的释放一氧化氮的衍生物作为抗肿瘤和抗炎药：设计，合成，生物学评估和一氧化氮释放研究。

设计和合成了一系列新的雷公藤内酯/呋喃丹杂种，作为雷公藤内酯类似物，雷公藤内酯是从雷神藤蔓（Tripterygium wilfordii Hook。F）中分离得到的天然化合物。这些合成的化合物中的一些在纳摩尔范围内显示出抗增殖活性。其中，化合物33具有良好的抗增殖活性和NO释放能力，并且化合物33的急性毒性比雷公藤内酯醇降低了160倍以上（LD50 = 160.9 mg / kg）。而且，化合物33以低剂量（0.3mg / kg）显着抑制黑素瘤的生长，并且在体外和体内显示出强的抗炎活性。这些结果表明化合物33可能是有希望的进一步研究的候选者。