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

被引:31
作者
Andreani, Aldo
Burnelli, Silvia
Granaiola, Massimiliano
Leoni, Alberto
Locatelli, Alessandra
Morigi, Rita
Rambaldi, Mirella
Varoli, Lucilla
Farruggia, Giovanna
Stefanelli, Claudio
Masotti, Lanfranco
Kunkel, Mark W.
机构
[1] Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy
[2] Univ Bologna, Dipartimento Biochim G Moruzzi, I-40126 Bologna, Italy
[3] NCI, Dev Therapeut Program, Informat Technol Branch, Div Canc Treatment & Diagnosis, Rockville, MD 20892 USA
关键词
D O I
10.1021/jm061077m
中图分类号
R914 [药物化学];
学科分类号
100701 [药物化学];
摘要
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.
引用
收藏
页码:7897 / 7901
页数:5
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