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ANTICANCER Pt(IV) COMPLEXES WITH LONIDAMINE AND BEXAROTENE LIGANDS: INFLUENCE OF LINKERтезисы доклада
- Авторы: Nosova Y.N., Zenin I.V., Maximova V.P., Zhidkova E.M., Kirsanov K.I., Milaeva E.R., Nazarov A.A.
- Сборник: 27th International Chugaev Conference on Coordination Chemistry
- Том: 1
- Тезисы
- Год издания: 2017
- Место издания: Nizhny Novgorod
- Первая страница: 353
- Аннотация: In cancer chemotherapy, drug combinations are almost general rule and platinum (IV) complexes may be considered as an ideal scaffold for incorporation of targeting ligand due to their stability and lower general toxicity. Conjugation with such ligands can increase the activity or selectivity of new complexes and lead to controlled release of an active organic molecule into cancer cell. In this work two series of Pt(IV) complexes with bioactive ligands were prepared. Glycolysis inhibitor lonidamine or retinoid X receptor agonist bexarotene were utilized as the bioactive ligands in cisplatin or oxaliplatin pharmacophore. In contrast to our previous work [1,2] ligands were introduced by using the mixed amide linker to separate metal center and organic drug. All synthetized compounds were characterized by NMR (1H, 13C, 195Pt, 15N) spectroscopy, ESI-MS and elemental analysis. The antiproliferative activity of the Pt(IV) complexes was investigated against several cancer cell lines (A549, SW480, MCF7). Most of complexes showed higher in vitro activity in comparison to lonidamine and bexarotene. Complex 2 exhibit low nanomolar cytotoxicity (IC50 0.7÷1.0 µM) and is notably more active than cisplatin.
- Добавил в систему: Окулова Юлия Николаевна