Studies on the Complexation of Platinum(II) by Some 4-Nitroisoxazoles and Testing the Cytotoxic Activity of the Resulting Complexes.

Two novel platinum(II) complexes ( and ) were synthesized by the reaction of the appropriate 3,5-dimethyl-4-nitroisoxazole with KPtCl and characterized by elemental analysis, ESI MS spectrometry, H NMR and far-IR spectroscopy. The structure of complex was additionally confirmed by X-ray diffraction. The cytotoxicity of the investigated compounds was examined in vitro on three human cancer cell lines (MCF-7 breast, ES-2 ovarian and A-549 lung adenocarcinomas) in both normoxia and hypoxia conditions.

Synthesis of Platinum(II) Complexes with Some 1-Methylnitropyrazoles and In Vitro Research on Their Cytotoxic Activity.

A series of eight novel platinum(II) complexes were synthesized by the reaction of the appropriate 1-methylnitropyrazole derivatives with KPtCl and characterized by elemental analysis, ESI MS spectrometry, H NMR, Pt NMR, IR and far IR spectroscopy. Thermal isomerization of -dichloridobis(1-methyl-4-nitropyrazole)platinum(II) to -dichloridobis(1-methyl-4-nitropyrazole)platinum(II) has been presented, and the structure of the compound has been confirmed by X-ray diffraction method. Cytotoxicity of the investigated compounds was examined in vitro on three human cancer cell lines (MCF-7 breast, ES-2 ovarian and A-549 lung adenocarcinomas) and their logP was measured using a shake-flask method.

Synthesis of new 1-phenyl-6H-pyrido[4,3-b]carbazole derivatives with potential cytostatic activity.

A number of new 1-substituted-6H-pyrido[4,3-b]carbazole derivatives have been synthesized. Nine of the newly obtained compounds were subjected to preliminary in vitro cytostatic activity screening against murine leukemia (L1210), human lung cancer (A549) and human colon cancer (HT29) cell lines. One particular compound 6f exhibited over 20 times better activity against L1210 tumor cell line than the reference ellipticine.

Synthesis and structure-activity relationship analysis of new olivacine derivatives.

The number of 3'- and 4'-substituted 1-phenyl-6H-pyrido[4,3-b]carbazole derivatives have been synthesized and tested biologically. Eleven of the newly obtained compounds were subjected to the preliminary cytostatic screening for their activity against L1210 (murine leukemia), A498 (human kidney cancer), A549 (human lung cancer) and HT29 (human colon cancer) cell lines. Eight of tested derivatives exhibited significant biological activities, which only weakly depended on side chain length and position of the substituent.

Synthesis and anticancer activity of new 1-substituted-6H-pyrido[4,3-b]carbazole derivatives.

This study examines the synthesis and cytostatic activity of new 5,6-dimethyl-1-substituted-6H-pyrido[4,3-b]carbazole derivatives. Their structures were confirmed by (1)H-NMR and elemental analysis. Seven of the new compounds were tested by the SRB method in vitro against human lung cancer (A549) and human kidney cancer (A498) cell lines.