Potential Antitumor Agents.: 42.: New antitumor imidazo[2,1-b]thiazole guanylhydrazones and analogues'

被引:146
作者
Andreani, Aldo [1 ]
Burnelli, Silvia [1 ]
Granaiola, Massimiliano [1 ]
Leoni, Alberto [1 ]
Locatelli, Alessandra [1 ]
Morigi, Rita [1 ]
Rambaldi, Mirella [1 ]
Varoli, Lucilla [1 ]
Calonghi, Natalia [2 ]
Cappadone, Concettina [2 ]
Farruggia, Giovanna [2 ]
Zini, Maddalena [2 ]
Stefanelli, Claudio [2 ]
Masotti, Lanfranco [2 ]
Radin, Norman S. [3 ]
Shoemaker, Robert H. [4 ]
机构
[1] Univ Bologna, Dipartimento Sci Farmaceut, I-40126 Bologna, Italy
[2] Univ Bologna, Dipartimento Biochim G Moruzzi, I-40126 Bologna, Italy
[3] Univ Michigan, Mol & Behav Neurosci Inst, Ann Arbor, MI 48109 USA
[4] Natl Canc Inst, Div Canc Treatment & Diagnosis, Dev Therapeut Program, Screening Technol Branch, Ft Detrick, MD 21702 USA
关键词
CELL-DEATH; INHIBITORS; APOPTOSIS;
D O I
10.1021/jm701246g
中图分类号
R914 [药物化学];
学科分类号
100705 [微生物与生化药学];
摘要
The synthesis of new antitumor 6-substituted imidazothiazole guanylhydrazones is described. Moreover, a series of compounds with a different basic chain at the 5 position were prepared. Finally, the replacement of the thiazole ring in the imidazothiazole system was also considered. All the new compounds prepared were submitted to the NCI cell line screen for evaluation of their antitumor activity. A few selected compounds were submitted to additional biological studies concerning effects on the cell cycle, apoptosis, and mitochondria.
引用
收藏
页码:809 / 816
页数:8
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