Culicinin D (1), a 10 amino acid peptaibol containing several unusual residues, has been shown to exhibit potent anticancer activity. Previous work in our group towards developing a structure-activity relationship (SAR) for this peptaibol has concentrated on replacement of the synthetically challenging AHMOD (3) and AMD (4) residues, resulting in the discovery of analogues with equivalent or better potency and simplified synthesis. The SAR of this peptaibol is extended in this work by investigating the effect of the N-terminal lipid tail and C-terminal amino alcohol, revealing the key contribution of each of these moieties on antiproliferative activity in a panel of breast and lung cancer cell lines.

Culicinin D（1）是一种含有10个氨基酸的肽醇，其中含有几个不同的残基，已显示出有效的抗癌活性。我们小组先前为开发该肽的构效关系（SAR）的工作主要集中在替代具有合成挑战性的AHMOD（3）和AMD（4）残基，从而发现了具有同等或更好效价且简化的类似物合成。通过研究N末端脂质尾巴和C末端氨基醇的作用，可扩展此肽酶的SAR ，从而揭示了这些部分对乳腺癌和肺癌细胞系中抗增殖活性的关键作用。