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STRUCTURE-ACTIVITY RELATIONSHIP OF COLCHICINOIDS BASED ON TUBULIN BINDING

STRUCTURE-ACTIVITY RELATIONSHIP OF COLCHICINOIDS BASED ON TUBULIN BINDING
基于微管蛋白结合的秋水仙碱类化合物的结构活性关系
批准号：
3855427
负责人：
A BROSSI
金额：
$0.0万
依托单位：
NATIONAL INSTITUTE OF DIABETES AND DIGESTIVE AND KIDNEY DISEASES
依托单位国家：
美国
项目类别：
财政年份：
--
资助国家：
美国
项目状态：
未结题
起止时间：
至
来源：
https://reporter.nih.gov/project-details/3855427
关键词：
N acylation antineoplastics chemical binding chemical structure function colchicine drug design /synthesis /production isothiocyanates neoplastic cell radiotracer tissue /cell culture tubulin

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英文摘要
Novel isothiocyanates of thiocolchicine and colchicine allocongeners were prepared as potential markers of the colchicine binding site on tubulin. The most interesting compound is 9-isothiocyanato-9-deoxy-N-acetylcolchinol which will be prepared in radiolabeled form to ensure specificity. Analogs of the potent inhibitor N-acetylcolchinyl methyl ether lacking methoxy groups at C(1), or at C(9), were found to be not very active. Several compounds of the colchicine series which showed good in vitro activity against human tumor cell lines will be tested in vivo.
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