Design and synthesis of molecular probes useful for the development of molecular-targeted chemotherapeutics for triple-negative breast cancer

SA-X是含有Phe（4-X）（X=Br，I）残基的N-甲基化环肽，对三阴性乳腺癌（TNBC）表现出有效的抗肿瘤活性。在这项研究中，我们设计并合成了分子探针，用于开发TNBC的分子靶向化疗药物。(1)SA-I成功地与生物素或荧光团标记的聚脯氨酸棒缀合。(2)通过锡-碘交换反应合成了放射性碘标记的SA-I（SA-[^<125>I]）。在<125>正常和荷瘤小鼠中给药后，SA-[^ I]在肝脏和肠道中显示出高蓄积。此外，SA-[^<125>I]在肿瘤中几乎不蓄积。

SA-X is a N-methylated cyclic peptide containing Phe(4-X)(X=Br, I) residue exhibiting potent antitumor activity against triple-negative breast cancer (TNBC). In this study, we designed and synthesized molecular probes useful for the development of molecular targeted chemotherapeutics for TNBC.(1) SA-I was successfully conjugated with biotin-or fluorophore-tagged polyproline rod.(2) Radioiodine-labeled SA-I (SA-[^<125>I]) was synthesized via tin-radioiodine exchange reaction. SA-[^<125>I] showed high accumulation in liver and intestine after administration to in normal and tumor-bearing mice. In addition, SA-[^<125>I] hardly accumulated in tumor.