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Syntheses and properties of selected derivatives of pyrimido[5,4-e]-l,3-thiazine and pyrimido[4,5-d]pyrimidine

100%

Malinka W. , Zawisza T. , Zajac H. E.

Archivum Immunologiae et Therapiae Experimentalis

1989

tom 37

nr 3-4

Rola lamelarnych warstw lipidowych w procesie przenikania substancji przez skórę

100%

Cieslik-Boczula K. , Jaszczyszyn A. , Swiatek P. , Malinka W.

Kosmetologia Estetyczna

2013

tom 02

nr 1

Antimutagenic activity of new analogues of fluphenazine

100%

Gasiorowski K. , Malinka W. , Swiatek P. , Jaszczyszyn A.

Cellular and Molecular Biology Letters

2003

tom 08

nr 4

Fluphenazine (FPh) exhibited antimutagenic activity in lymphocyte cultures, markedly decreasing genotoxic effects of standard mutagenic agents present in cell cultures. However, the strong pharmacological activity of this neuroleptic drug, together with its serious side effects on the central nervous system, limits its use as an antimutagenic compound. In this paper we describe a route of chemical synthesis of FPh analogues that are more hydrophilic than the model compound, thus probably penetrate more weakly through the blood-brain barrier. These new analogues were tested for their antimutagenic and pro-apoptotic activities in human lymphocyte cultures, genotoxically damaged in vitro with benzo[a]pyrene [40 μM, 30 min] and subsequently cultured for 48 h in the presence of the tested compounds. The fluphenazine analogues enhanced apoptosis in genotoxically damaged lymphocytes more strongly than the model compound did. The increase of apoptotic cell frequency was the highest with compound 4a [2-(trifluoromethyl)-10-[3-(diethanolamino)-2-hydroxypropyl] phenothiazine] - a 35% higher effect than that of fluphenazine. The cytotoxicity of derivative 4a was the lowest among the tested compounds; it was 60% lower than that of fluphenazine. The antimutagenic effect of 4a was about 10% stronger than that of fluphenazine. Compund 4a also had the highest hydrophilicity of the new FPh analogues. Compound 4a was chosen for further study as a potentially usable antimutagen that would only weakly penetrate the central nervous system.

Induction of apoptosis through oxidative stress-related pathway in multidrug-resistant colon cancer cells by oxicam derivatives

88%

Sroda-Pomianek K. , Szczesniak-Siega B. , Wesolowska O. , Malinka W. , Michalak K.

Current Topics in Biophysics. Supplement

2016

tom 39

nr A: Plenary lectures

Studies on Reactions of 3-Benzoyl-4-hydroxypyrido[3,2-e)-1,2-thiazines with Primary Amines and N-Methylhydrazine

88%

Malinka W. , Karczmarczyk Z. , Kaczmarz M. , Świątek P. , Urbańczyk-Lipkowska Z.

Polish Journal of Chemistry

2004

tom Vol. 78 / nr 6

815-829

Reaction of the appropriate 3-benzoyl-4-hydroxypyrido[3,2-e]-1,2-thiazine-1,1-dioxides 2 bearing a methyl or a 3-(4-arylpiperazin-1-yl)propyl group at the nitrogen atom of the thiazine ring with primary amines resulted in enamines of type (E)-3. The related products 8 were obtained by alkylation of 3-phenylpyrazolo[4,3-c]pyrido[3,2-e]-1,2- thiazine-5,5-dioxide 7 with the corresponding 1-aryl-4-(3-chloropropyl)piperazines 9. The structures of the new heterocycles 3 and8, synthesized for pharmaceutical purposes, and of the model compounds 4-6, prepared for comparison of spectral properties, were proven through elemental, IR, 1H NMR and, in some cases (3d, 8a), X-ray data.

Activity of newly synthesized phenothiazine derivatives as antiproliferative and MDR reversing agents in colon cancer cells

75%

Sroda-Pomianek K. , Swiatek P. , Wesolowska O. , Pola A. , Malinka W. , Michalak K.

Current Topics in Biophysics. Supplement

2013

tom 36

nr 2A: Posters