A series of natural aristolactams and their analogues have been prepared and evaluated for antitumor activity against human cancer cells, including multi-drug resistant cell lines. Naturally occurring aristolactams, such as aristolactam BII (cepharanone B), aristolactam BIII, aristolactam FI (piperolactam A), N-methyl piperolactam A, and sauristolactam showed moderate antitumor activities in selected cell lines. However, several synthetic aristolactam derivatives exhibited potent antitumor activities against a broad array of cancer cell lines with GI₅₀ values in the submicromolar range.

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马兜铃内酰胺类似物的合成及其抗肿瘤活性的评价

已经制备了一系列天然马兜铃内酰胺及其类似物，并评估了其对人类癌细胞（包括多药耐药细胞系）的抗肿瘤活性。天然存在的马兜铃内酰胺，例如马兜铃内酰胺BII（头孢兰酮B），马兜铃内酰胺BIII，马兜铃内酰胺FI（哌内酰胺A），N-甲基哌内酰胺A和sauristolactam在选定的细胞系中显示中等的抗肿瘤活性。然而，几种合成的马兜铃内酰胺衍生物对亚微摩尔范围内的GI ₅₀值的多种癌细胞表现出有效的抗肿瘤活性。