Nazarov Alexey A, Baquié Mathurin, Nowak-Sliwinska Patrycja, Zava Olivier, van Beijnum Judy R, Groessl Michael, Chisholm Danielle M, Ahmadi Zohrab, McIndoe J Scott, Griffioen Arjan W, van den Bergh Hubert, Dyson Paul J
1] Institute of Chemical Sciences and Engineering, Swiss Federal Institute of Technology (EPFL), CH-1015 Lausanne, Switzerland [2] Department of Chemistry, Moscow State University, Leninskie Gory, 119991, Moscow, Russia.
Sci Rep. 2013;3:1485. doi: 10.1038/srep01485.
New triruthenium-carbonyl clusters derivatized with glucose-modified bicyclophosphite ligands have been synthesized. These compounds were found to have cytostatic and cytotoxic activity and depending on the number of bicyclophosphite ligands, and could be tuned for either anti-cancer or specific anti-angiogenic activity. While some compounds had a broad cellular toxicity profile in several cell types others showed endothelial cell specific dose-dependent anti-proliferative and anti-migratory efficacy. A profound inhibition of angiogenesis was also observed in the in vivo chicken chorioallantoic membrane (CAM) model, and consequently, these new compounds have considerable potential in drug design, e.g. for the treatment of cancer.
已合成了用葡萄糖修饰的双环亚磷酸酯配体衍生的新型三钌羰基簇合物。发现这些化合物具有细胞生长抑制和细胞毒性活性，并且根据双环亚磷酸酯配体的数量，可以调节其抗癌或特定的抗血管生成活性。虽然一些化合物在几种细胞类型中具有广泛的细胞毒性谱，但其他化合物显示出内皮细胞特异性剂量依赖性抗增殖和抗迁移功效。在体内鸡胚绒毛尿囊膜（CAM）模型中也观察到了对血管生成的显著抑制，因此，这些新化合物在药物设计中具有相当大的潜力，例如用于癌症治疗。
