Molecular Targets Laboratory, Center for Cancer Research, National Cancer Institute, Frederick, Maryland 21702, USA.
Org Lett. 2011 Jul 1;13(13):3518-21. doi: 10.1021/ol201329p. Epub 2011 Jun 6.
Extracts of the sponge genus Candidaspongia showed selective cytotoxicity toward melanoma cells in the NCI 60-cell-line screen. Continued investigation of the Candidaspongia sp. extracts led to the isolation of three new tedanolide analogues, precandidaspongiolides A (1) and B (2) and candidaspongiolide B (4), as well as candidaspongiolide A (3) and tedanolide (5). Semisynthetic derivatives were also generated to develop SAR. Candidaspongiolides A/B were the most potent and showed low nanomolar activity against several melanoma cell lines.
海绵属 Candidaspongia 的提取物对 NCI 60 细胞系筛选中的黑色素瘤细胞具有选择性细胞毒性。对 Candidaspongia sp.提取物的进一步研究导致了三种新的 Tedanolide 类似物，即 precandidaspongiolides A（1）和 B（2）以及 candidaspongiolide B（4），以及 candidaspongiolide A（3）和 Tedanolide（5）的分离。还生成了半合成衍生物以开发 SAR。Candidaspongiolides A/B 是最有效的，对几种黑色素瘤细胞系表现出低纳摩尔的活性。
