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Pregled bibliografske jedinice broj: 152577

Zbornik radova

Autori: Barbarić, Monika; Uršić, Stanko; Pilepić, Viktor; Zorc, Branka; Hergold-Brundić, Antonija; Nagl, Ante; Grdiša, Mira; Pavelić, Krešimir; Snoeck, Robert; Andrei, Graciela; Balzarini, Jan; De Clercq, Erik; Mintas, Mladen
Naslov: Synthesis, X-Ray Crystal Structure Study, Cytostatic and Antiviral Evaluation of the Novel Cycloalkyl-N-aryl-hydroxamic Acids
Izvornik: Drugs of the Future / Prous, J.R. (ur.). - Copenhagen :
Skup: XVIIIth International Symposium on Medicinal Chemistry
Mjesto i datum: Copenhagen, Danska ; Malmo, Švedska, 15-19.08.2004.
Ključne riječi: Cycloalkyl-N-aryl-hydroxamic acids; Cytostatic and Antiviral Evaluation; 1H and 13C NMR study
Sažetak:
The novel cycloalkyl-N-(4-chlorophenyl)-hydroxamic acids (2a-f) were synthesized by a specific approach which enabled a direct introduction of chloro substituent in the benzene ring, using acyl chloride and nitrosobenzene as starting reagents. The nonhalogenated compound 2g was prepared from the corresponding acyl chloride and N-phenylhydroxylamine. The structures of the compounds were deduced from their 1H and 13C NMR spectra. An unequivocal proof of the structure and conformation of 2d was established by X-ray crystallographic analysis. Compounds 2b, d, e and g exhibited rather marked inhibitory activity (IC50 = 7-80 mM) against malignant tumor cell lines: colon carcinoma (SW620), laryngeal carcinoma (Hep2), pancreatic carcinoma (MiaPaCa2), breast carcinoma (MCF7) and cervical carcinoma (HeLa), but also against human normal fibroblasts (WI38). The best selectivity against tumor cell lines vs. normal fibroblasts was shown by compounds 2a and 2c. Compound 2e showed the most pronounced anti-CMV activity (EC50 = 1.5 and 0.8 mg mL-1) only at ≥ 5-fold lower than the cytotoxic concentration. Compounds 2d and 2f showed modest, albeit selective activity against cytomegalovirus (2d: EC50 = 7.3-8.9 mg mL-1, selectivity index 7-10, and 2f: EC50 = 7-13 mg mL-1 and selectivity index 10). These compounds represent therefore anti-CMV leads for further synthetic optimization.
Vrsta sudjelovanja: Poster
Vrsta prezentacije u zborniku: Sažetak
Vrsta recenzije: Međunarodna recenzija
Projekt / tema: 0125003, 0006543
Izvorni jezik: ENG
Kategorija: Znanstveni
Znanstvena područja:
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