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放线菌素是一类具有良好抗肿瘤作用而有较大毒性的抗菌素。作者等推测放线菌素的抗癌作用与其共有的色基结构有较为密切的关系,而环肽部分可能起一种载体作用。基于上述设想,我们曾合成了一系列有关化合物试验其抗肿瘤作用。其中发现放线菌素色基与叶酸的二肽部分结合的化合物具有明显的抗肿瘤作用。本文继续报道将放线菌素的环肽部分调换为简单的二肽、三肽或五肽的化合物;用丝氨酸代替苏氨酸,用甘氨酸和N-甲基甘氨酸代替其他氨基酸。共合成了七个化合物(2～8)。
Actinomycin is a class of antibiotics with good anti-tumor effects and greater toxicity. The authors speculate that actinomycin anti-cancer effect and its common color-based structure has a closer relationship, while the part of the cyclic peptide may play a carrier role. Based on the above assumptions, we have synthesized a series of related compounds to test their anti-tumor effect. Among them, it was found that the compound having the actinomycin-based moiety and the dipeptide moiety of folic acid had a significant anti-tumor effect. This article continues to report the replacement of the cyclic peptide moiety of actinomycin with a simple dipeptide, tripeptide or pentapeptide compound; substitution of threonine with serine and substitution of glycine and N-methylglycine for other amino acids. A total of seven compounds were synthesized (2 ~ 8).