A novel conjugate between a cyclometalated platinum(II) complex with dual antiangiogenic and antitumor activity and a cyclic peptide containing the RGD sequence (‐Arg‐Gly‐Asp‐) has been synthesized by combining solid‐ and solution‐phase methodologies. Although peptide conjugation rendered a non‐cytotoxic compound in all tested tumor cell lines (± α_Vβ₃ and α_Vβ₅ integrin receptors), the antiangiogenic activity of the Pt‐c(RGDfK) conjugate in human umbilical vein endothelial cells at sub‐cytotoxic concentrations opens the way to the design of a novel class of angiogenesis inhibitors through conjugation of metallodrugs with high antiangiogenic activity to cyclic RGD‐containing peptides or peptidomimetic analogues.

中文翻译：

---

基于金属有机铂（II）配合物与RGD肽共轭的血管生成抑制剂。

通过结合固相和溶液相方法，合成了具有双重抗血管生成和抗肿瘤活性的环金属化铂（II）复合物与包含RGD序列的环肽（‐Arg‐Gly‐Asp‐）之间的新型共轭物。虽然肽缀合呈现在所有测试的肿瘤细胞系的非细胞毒性化合物（±α _V β ₃，α _V β ₅中的人整联受体）时，Pt-C的抗血管生成活性（RGDfK）缀合物脐静脉内皮在子细胞通过将具有高抗血管生成活性的金属药物与含环状RGD的肽或拟肽类似物缀合，细胞毒性浓度为新型血管生成抑制剂的设计开辟了道路。