Design and synthesis of the inhibitors for chemokine receptor CCR5

Callipeltins是Zampella等人从海绵中分离得到的一类线性和环状缩酚酸肽。据报道，这些分子表现出抗HIV活性和对各种肿瘤细胞系的细胞毒性。在我们最近关于环状缩酚肽的合成研究的研究过程中，我们进行了关于callipeltins的合成的研究，callipeltins被认为是作为抗HIV药物或抗癌剂的CCR 5抑制剂的有效结构。在本研究中，我们进行了立体选择性合成的几个不常见的氨基酸和callipeltin E，M和B的固相Fmoc策略合成。此外，我们评估了对Hela细胞系的细胞毒性。

Callipeltins are linear-and cyclic depsi-peptides isolated from marine sponge by Zampella's group. These molecules were reported to exhibit anti-HIV activity and cytotoxicity against various tumor cell lines. In the course of our recent research regarding the synthetic study of cyclic depsipeptides, we conducted studies on the synthesis of callipeltins supposed to be efficient structures for CCR5 inhibitors as anti-HIV drugs or anti-cancer agents. In the present study, we performed the stereoselective synthesis of several unusual amino acids and solid phase synthesis of callipeltin E, M and B on Fmoc-strategy. In addition, we evaluated the cytotoxicity against the Hela cell line.