Wynik wyszukiwania w bazie Polska Bibliografia Lekarska GBL
Zapytanie:
GOLANKIEWICZ
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2
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Tytuł oryginału:
In vitro cytostatic activity of 8-substituted and tricyclic analogues of acyclovir.
Autorzy:
Hładoń
Bogusław,
Gośliński
Tomasz,
Laskowska
Halina,
Baranowski
Daniel,
Ostrowski
Tomasz,
Zeidler
Joanna,
Ruszkowski
Piotr,
Golankiewicz
Bożenna
Źródło:
Pol. J. Pharmacol. 2002: 54 (1) s.45-53, il., tab., bibliogr. 22 poz.
Sygnatura GBL:
313,156
Hasła klasyfikacyjne GBL:
farmacja
onkologia
Typ dokumentu:
praca doświadczalna
tytuł obcojęzyczny
Wskaźnik treści:
ludzie
in vitro
Streszczenie angielskie:
Out of a series of twenty 8-substituted or/and 1,N-2-bridged (tricyclic) derivatives of acyclovir (a selective antiherpetic drug), known to be nontoxic to normal cells, seven compounds were found to exhibit moderate cytostatic activity in KB human tumor tissue culture system with ED50 activity values ranging from 0.052-0.094 x 10**-3 mole/l. The structure-activity relationship analysis indicated that the primary factors determining their cytotoxicity were: 1) bromine atom at the C-8 position of the bicyclic derivatives and 2) unsubstituted appended ring in the tricyclic derivatives. Combination of two structural elements carrying the cytotoxicity gave diverse effects, enhancement or decrease in activity depending on particular cases. Two compounds (of four selected), 8-bromoacyclovir and 1,N-2-ethenoacyclovir, having unsubstituted 9-[(2-hydroxyethoxy)methyl] chain, showed approximately 2-fold increase in their cytotoxicity against HeLa tumor cells in the presence of the induced microsomal generating system suggesting that their cytooxicity depends on the drug metabolic transformation into their active metabolites (intermediates) via MFO-system, and that structural unit of this chain is essential for abovementioned activation. Presently found remarkable cytotoxic selectivity of acyclovir analogues against KB and HeLa tumor cells together with previously reported in the literature specific cytotoxic activity of acyclovir against murine leukemia L1210 cells seem to be encouraging for further investigation of this class of compounds in other tumor systems.
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Tytuł oryginału:
Synthesis and biological activity of strongly fluorescent tricyclic analogues of acyclovir and ganciclovir.
Autorzy:
Goslinski
Tomasz,
Golankiewicz
Bożenna,
De Clercq
Erik,
Balzarini
Jan
Źródło:
J. Med. Chem. 2002: 45 (23) s.5052-5057, il., tab., bibliogr. 13 poz.
Sygnatura GBL:
312,133
Hasła klasyfikacyjne GBL:
farmacja
Typ dokumentu:
praca doświadczalna
praca opublikowana za granicą
tytuł obcojęzyczny
Streszczenie angielskie:
In search of strongly fluorescent tricyclic analogues of acyclovir (ACV, 1) and ganciclovir (GCV, 2) derivatives of the 3,9-dihydro-9-oxo-5H-imidazo[1,2-ŕ]purine system, several 6-[4-(acyloxy)-phenyl], 6-[4-(acylamino)phenyl], and 6-[4-(phenoxycarbonyloxy)phenyl]-substituted TACV and TGCV analogues were synthesized and evaluated for their activity against herpes simplex virus types 1 and 2 in cell culture. All TACV and TGCV analogues showed strong fluorescence (quantum yield of 30-65 p.c. vs 2-aminopurine 100 p.c.). The 6-[4-(phenoxycarbonyloxy)phenyl]-substituted compounds 11 and 19 displayed the best combination of the fluorescence and antiviral potency.
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