2. Academic Validation
  3. Synthesis, X-ray crystal structure study, and cytostatic and antiviral evaluation of the novel cycloalkyl-N-aryl-hydroxamic acids

Synthesis, X-ray crystal structure study, and cytostatic and antiviral evaluation of the novel cycloalkyl-N-aryl-hydroxamic acids

  • J Med Chem. 2005 Feb 10;48(3):884-7. doi: 10.1021/jm040878r.
Monika Barbarić 1,  Stanko Ursić,  Viktor Pilepić,  Branka Zorc,  Antonija Hergold-Brundić,  Ante Nagl,  Mira Grdisa,  Kresimir Pavelić,  Robert Snoeck,  Graciela Andrei,  Jan Balzarini,  Erik De Clercq,  Mladen Mintas
Affiliations

Affiliation

  • 1 Faculty of Pharmacy and Biochemistry, University of Zagreb, 10000 Zagreb, Croatia. mlovrek@yahoo.com
PMID: 15689173 DOI: 10.1021/jm040878r
Abstract

In vitro evaluation of the novel cycloalkyl-N-(4-chlorophenyl)-hydroxamic acids (2a-g) demonstrated that 2b,d,e exhibited rather marked inhibitory activity (IC50 = 7-10 microM) against pancreatic carcinoma, 2b-d against colon carcinoma, 2d against laryngeal carcinoma, and 2b,d against breast carcinoma. 2e showed the most pronounced anti-cytomegalovirus activity (EC50 = 1.5 and 0.8 microg mL(-1)) only at > or = 5-fold lower than the cytotoxic concentration. 2d and 2f showed modest, albeit selective, activity against cytomegalovirus (2d, EC50 = 7.3-8.9 microg mL(-1), selectivity index 7-10; 2f, EC50 = 7-13 microg mL(-1), selectivity index 10).

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