Depart. de Q. Inorgánica y Orgánica, Univ. Jaume I, Avda. Sos Baynat s/n, 12071 Castellón, Spain.
Chemistry. 2011 Jan 10;17(2):675-88. doi: 10.1002/chem.201001682. Epub 2010 Nov 9.
Total, stereoselective syntheses of the naturally occurring, cytotoxic macrolides aspergillide A and B are described. Olefin metatheses and asymmetric allylations were key steps in the synthetic sequences. Cytotoxicity assays against several tumor cell lines have been performed for the two aspergillides and some of the intermediates or side products of the synthetic sequence. One of these intermediates has been found markedly active against the human leukemia cancer cell line HL-60, with an IC(50) value comparable with that of the clinical drug fludarabine.
本文描述了天然细胞毒素大环内酯aspergillide A 和 B 的全立体选择性合成。烯烃复分解和不对称烯丙基化是合成序列中的关键步骤。对两种aspergillides 以及合成序列的一些中间体或副产物进行了针对几种肿瘤细胞系的细胞毒性测定。其中一种中间体对人白血病癌细胞系 HL-60 表现出明显的活性，其 IC（50）值与临床药物氟达拉滨相当。
