The design and synthesis of antitumor imidazothiazole guanylhydrazones are reported. The compounds were submitted to NCI for testing. All but one were more active than methyl-GAG. A few compounds were selected for further studies in search of a possible mechanism of action. The results from these studies and a final search with the NCI COMPARE algorithm suggest that the guanylhydrazones described in this paper are acting through a novel mechanism of action.
A. Andreani, S. Burnelli, M. Granaiola, A. Leoni, A. Locatelli, R. Morigi, et al. (2006). Synthesis and antitumor activity of Guanylhydrazones from 6-(2,4-dichloro-5-nitrophenyl)imidazo[2,1-b]thiazoles and 6-pyridylimidazo[2,1-b]thiazoles. JOURNAL OF MEDICINAL CHEMISTRY, 49, 7897-7901 [10.1021/jm061077m].
Synthesis and antitumor activity of Guanylhydrazones from 6-(2,4-dichloro-5-nitrophenyl)imidazo[2,1-b]thiazoles and 6-pyridylimidazo[2,1-b]thiazoles
ANDREANI, ALDO;BURNELLI, SILVIA;GRANAIOLA, MASSIMILIANO;LEONI, ALBERTO;LOCATELLI, ALESSANDRA;MORIGI, RITA;RAMBALDI, MIRELLA;VAROLI, LUCILLA;FARRUGGIA, GIOVANNA;STEFANELLI, CLAUDIO;MASOTTI, LANFRANCO;
2006
Abstract
The design and synthesis of antitumor imidazothiazole guanylhydrazones are reported. The compounds were submitted to NCI for testing. All but one were more active than methyl-GAG. A few compounds were selected for further studies in search of a possible mechanism of action. The results from these studies and a final search with the NCI COMPARE algorithm suggest that the guanylhydrazones described in this paper are acting through a novel mechanism of action.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
