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Anticancer activity of cytokinins: structure-activity relationship studies
Údaje o názvu Anticancer activity of cytokinins: structure-activity relationship studies [rukopis] / Jiří Voller Další variantní názvy Protinádorová aktivita cytokininů: Studie vztahu mezi strukturou a účinkem Osobní jméno Voller, Jiří (autor diplomové práce nebo disertace) Překl.náz Anticancer activity of cytokinins: structure-activity relationship studies Vyd.údaje 2010 Fyz.popis 32 s. (50646) , 35 s. prilohy + 1 ks CD ROM Poznámka Ved. práce Miroslav Strnad Dal.odpovědnost Strnad, Miroslav, 1958- (vedoucí diplomové práce nebo disertace) Kovařík, Jan (oponent) Santaniello, Enzo (oponent) Mlejnek, Petr (oponent) Dal.odpovědnost Univerzita Palackého. Katedra botaniky (udelovatel akademické hodnosti) Klíč.slova SAR * cytokinins * cancer * ortho-topolin riboside * NCI60 * SAR * cytokinins * cancer * ortho-topolin riboside * NCI60 Forma, žánr disertace dissertations MDT (043.3) Země vyd. Česko Jazyk dok. angličtina Druh dok. PUBLIKAČNÍ ČINNOST Titul Ph.D. Studijní program Doktorský Studijní program Biologie Studijní obor Botanika kniha
Kvalifikační práce Staženo Velikost datum zpřístupnění 130906-216137836.pdf 33 973.6 KB 24.06.2010 Signatura Čár.kód Lokace Dislokace Info DIS/082 (PřF-KBO) 3134512114 PřF-Holice PřF, Knihovna Holice - sklad pouze prezenčně
A study of the relationship between the chemical structure of cytokinins and their cytotoxic effects against a panel of human cancer cell lines with diverse histopathological origins is presented. Test compounds included almost all known natural cytokinins (N = 42) and two groups of novel synthetic analogues: derivatives of N6-benzyladenosine with diverse substitutions on the benzyl ring (N = 48) and their analogues where the ribose moiety is replaced by a tetrahydropyran-2-yl or tetrahydrofuran-2-yl group (N = 34). Strong cytotoxic activity was limited to certain cytokinin ribosides and their corresponding ribotides. The anticancer activity of aromatic cytokinin ribosides can be improved by fluorination or ortho- hydroxylation of the benzyl ring. The potent anticancer activity of the natural cytokinin ortho-topolin riboside (median GI50 = 0.65 ?M) was confirmed using NCI60. Its activity pattern was distinctly different from those of standard anticancer drugs, suggesting that it has a unique mechanism of action. In comparison with standard drugs, ortho-topolin riboside showed exceptional cytotoxic activity against NCI60 cell lines with a mutated p53 tumour suppressor gene. Ortho-topolin riboside also exhibited significant anticancer activity against several tumour models in in vivo hollow fibre assays.A study of the relationship between the chemical structure of cytokinins and their cytotoxic effects against a panel of human cancer cell lines with diverse histopathological origins is presented. Test compounds included almost all known natural cytokinins (N = 42) and two groups of novel synthetic analogues: derivatives of N6-benzyladenosine with diverse substitutions on the benzyl ring (N = 48) and their analogues where the ribose moiety is replaced by a tetrahydropyran-2-yl or tetrahydrofuran-2-yl group (N = 34). Strong cytotoxic activity was limited to certain cytokinin ribosides and their corresponding ribotides. The anticancer activity of aromatic cytokinin ribosides can be improved by fluorination or ortho- hydroxylation of the benzyl ring. The potent anticancer activity of the natural cytokinin ortho-topolin riboside (median GI50 = 0.65 ?M) was confirmed using NCI60. Its activity pattern was distinctly different from those of standard anticancer drugs, suggesting that it has a unique mechanism of action. In comparison with standard drugs, ortho-topolin riboside showed exceptional cytotoxic activity against NCI60 cell lines with a mutated p53 tumour suppressor gene. Ortho-topolin riboside also exhibited significant anticancer activity against several tumour models in in vivo hollow fibre assays.
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