Čeština
EnglishNovel platinum(II) and palladium(II) complexes with cyclin-dependent kinase inhibitors: Synthesis, characterization and antitumour activity
Szüčová, Lucie; Trávníček, Zdeněk; Zatloukal, Marek; Popa, Igor
BIOORGANIC AND MEDICAL CHEMISTRY 14 [2]: 479-491, 2006
Keywords: Platinum(II); Palladium(II); Cyclin-dependent kinase inhibitors
Abstract: The Pt(H) and Pd(II) complexes of the types cis-[Pt(L-1)(2)Cl-2]center dot H2O (1), cis-[Pt(L-2)(2)Cl-2]center dot 3H(2)O (2), trans- [Pd(L-1)(2)Cl-2]center dot H2O (3), trans-[Pd(L2)(2)Cl-2]center dot H2O (4), trans-[Pd(L-3)(2)Cl-2]2DMF (5) and trans-[Pd(L-4)(2)Cl-2]2DMF (6) (L-1-L-4 = cyclin-dependent kinase inhibitors derived from 6-benzylamino-9-isopropylpurine) have been prepared and characterized. The complexes have been studied by elemental analyses, conductivity measurements, ES+ MS, FT-IR, H, C-13 and Pt-195 NMR spectra, differential scanning calorimetry and thermogravimetric analysis. The molecular structures of L-1, trans-[Pd(L-3)(2)Cl-2](.)2DMF (5) and trans- [Pd(L-4)(2)Cl-2](.)2DMF (6) have been determined by single crystal X-ray analysis. The complexes have been tested in vitro due to their presumable anticancer activity against the following human cancer cell lines: K-562, MCF7, G-361 and HOS. Satisfying results were obtained for the complex 1 with IC50 values of 6 mu M acquired against G-361 as well as against HOS cell lines. The lowest values of IC50 were achieved for the complexes 3 and 4 against MCF 7 cell line with IC50 3 mu M (for 3) and also 3 mu M (for 4).
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IEB authors: bývalý zaměstnanec
BIOORGANIC AND MEDICAL CHEMISTRY 14 [2]: 479-491, 2006
Keywords: Platinum(II); Palladium(II); Cyclin-dependent kinase inhibitors
Abstract: The Pt(H) and Pd(II) complexes of the types cis-[Pt(L-1)(2)Cl-2]center dot H2O (1), cis-[Pt(L-2)(2)Cl-2]center dot 3H(2)O (2), trans- [Pd(L-1)(2)Cl-2]center dot H2O (3), trans-[Pd(L2)(2)Cl-2]center dot H2O (4), trans-[Pd(L-3)(2)Cl-2]2DMF (5) and trans-[Pd(L-4)(2)Cl-2]2DMF (6) (L-1-L-4 = cyclin-dependent kinase inhibitors derived from 6-benzylamino-9-isopropylpurine) have been prepared and characterized. The complexes have been studied by elemental analyses, conductivity measurements, ES+ MS, FT-IR, H, C-13 and Pt-195 NMR spectra, differential scanning calorimetry and thermogravimetric analysis. The molecular structures of L-1, trans-[Pd(L-3)(2)Cl-2](.)2DMF (5) and trans- [Pd(L-4)(2)Cl-2](.)2DMF (6) have been determined by single crystal X-ray analysis. The complexes have been tested in vitro due to their presumable anticancer activity against the following human cancer cell lines: K-562, MCF7, G-361 and HOS. Satisfying results were obtained for the complex 1 with IC50 values of 6 mu M acquired against G-361 as well as against HOS cell lines. The lowest values of IC50 were achieved for the complexes 3 and 4 against MCF 7 cell line with IC50 3 mu M (for 3) and also 3 mu M (for 4).
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