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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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中文摘要
翻译
硫代秋水仙碱和秋水仙碱同种异体的新型异硫氰酸酯， 制备作为微管蛋白上秋水仙素结合位点的潜在标记物。 最有趣的化合物是9-异硫氰酸基-9-脱氧-N-乙酰秋水仙醇 其将以放射性标记的形式制备以确保特异性。 类似物 强效抑制剂N-乙酰秋水仙素甲基醚缺乏甲氧基 在C（1）或C（9）的基团被发现不是很活跃。 几 秋水仙碱系列化合物显示出良好的体外活性， 将在体内测试针对人肿瘤细胞系的抗体。
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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