Synthesis, characterization and antitumor activity of novel octahedral Pt(IV) complexes.
作者： Young-Ee Kwon , Kyu-Ja Whang , Young-Ja Park , Kuk Hwan Kim
DOI: 10.1016/S0968-0896(03)00044-0
关键词: Chemical synthesis 、 Nuclear magnetic resonance spectroscopy 、 Chemistry 、 Carboxylate 、 Molecule 、 Octahedron 、 Stereochemistry 、 Platinum 、 Malonate 、 Diamine
摘要: Novel platinum(IV) complexes were synthesized having octahedral structure for new antitumor agents. The series of (1,4-butanediamine)Pt(IV) the type trans,cis-[PtA(2)Cl(2)(1,4-butanediamine)] (A=hydroxo 9, acetato 12, trifluoroacetato 13 as axial ligands) and trans-[PtA(2)(malonate)(1,4-butanediamine)] 16, 17, 18) characterized by IR, NMR elemental analysis. molecular structures 18 have been determined X-ray diffraction methods. crystals are monoclinic, P2 1/c with a=21.165 (5), b=9.050 (3), c=15.293 (3) A, beta=103.89 (2) degrees Z=8 a=10.178 b=12.894 (9), c=12.182 (8) beta=91.01 (5) Z=4 a=10.460 b=11.199 (8), c=15.641 (7) beta=98.41 degrees, 18. Three crystallographically independent molecules coordination around Pt(IV) cation. prepared acetylation or trifluoroacetylation trans,cis-[Pt(OH)(2)Cl(2)(1,4-butanediamine)]. trans-[PtA(2)malonate(1,4-butanediamine)] 17 was a similar method. in vitro cytotoxicity theses evaluated against 12 cancer cell lines assayed MTS IC(50) values compounds shown to be lower than those cisplatin. vivo activity using mice bearing L1210 leukemia, B16 melanoma L1210/cis-DDP animal models. compound found highest cisplatin-resistant cells, L1210/cis-DDP, vivo.
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