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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：
3876467
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/3876467
关键词：
N acylation antineoplastics binding proteins chemical binding chemical structure function colchicine cycloalkene deuterium drug design /synthesis /production esters isothiocyanates thioether thiones tubulin

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英文摘要
Amides of deacetylcolchicine and deacetylisocolchicine with dihydrofluorescein diacetate have been prepared as potential markers of the colchicine binding site on tubulin. (14)C-labeled isothiocyanato- deacetylthiocolchicine did not prove to be useful to specifically mark the colchicine binding site. Total synthesis of two ring A dimethoxy substituted dibenzocycloheptatrienes revealed that all 3 methoxy groups in the ring A of colchicine are important for the interaction with proteins. Optically active isomers of N-acetyl- colchinol methyl ether with the acetamido group at C(5) did not bind to tubulin.
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