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某些取代的5-哒嗪基-苯乙烯基酮的体外抗肿瘤活性的合成与评价

Synthesis and evaluation of in vitro antitumor activity of some substituted 5-pyridazinyl-styrylketones.

作者信息

Ciciani G, Dal Piaz V, Giovannoni M P

机构信息

Dipartimento di Scienze Farmaceutiche, Facoltà di Farmacia, Università di Firenze.

出版信息

Farmaco. 1991 Jul-Aug;46(7-8):873-85.

PMID:1793472
Abstract

A series of twenty pyridazinyl-styrilketones, substituted at position 4 with linear or cyclic tertiary amino groups, were synthesized and evaluated in vitro as antitumor agents against 60 human tumor cell-lines. Moderate activity and differential cell sensitivity were found for several of the compounds. Cell-line XF-498L (panel:Brain) showed differential cell sensitivity towards compound 5b (more than 1000 times the mean sensitivity of all cell-lines).

摘要

合成了一系列20种在4位被直链或环状叔氨基取代的哒嗪基-苯乙烯基酮,并作为抗肿瘤剂在体外针对60种人类肿瘤细胞系进行了评估。发现其中几种化合物具有中等活性和不同的细胞敏感性。细胞系XF-498L(类别:脑)对化合物5b表现出不同的细胞敏感性(超过所有细胞系平均敏感性的1000倍)。

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