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苯并咪唑稠环体系。十一。一些具有预期抗肿瘤活性的取代环烷基吡啶并[1,2 - a]苯并咪唑的合成。

Benzimidazole condensed ring systems. XI. Synthesis of some substituted cycloalkyl pyrido[1,2-a]benzimidazoles with anticipated antineoplastic activity.

作者信息

Badawey E A, Kappe T

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, AR, Alexandria, Egypt.

出版信息

Eur J Med Chem. 1999 Jul-Aug;34(7-8):663-7. doi: 10.1016/s0223-5234(00)80036-7.

Abstract

As part of a research project on the synthesis of a number of pyrido[1,2-a]benzimidazole derivatives with possible antineoplastic activity, and as a result of the interesting antineoplastic activity recorded for one such compound (NSC 649900), some new cycloalkylpyrido[1,2-a]benzimidazoles were prepared and evaluated for such activity. Compound (7c, NSC 682011) exhibited a good in vitro antineoplastic activity especially against most of the leukaemia cell lines. This compound has been selected by the NCI for further testing in a new in vivo anticancer hollow fibre assay.

摘要

作为一个关于合成多种可能具有抗肿瘤活性的吡啶并[1,2-a]苯并咪唑衍生物的研究项目的一部分,并且由于记录到一种此类化合物(NSC 649900)具有有趣的抗肿瘤活性,制备了一些新的环烷基吡啶并[1,2-a]苯并咪唑并对其抗肿瘤活性进行了评估。化合物(7c,NSC 682011)表现出良好的体外抗肿瘤活性,尤其是对大多数白血病细胞系。美国国立癌症研究所已选择该化合物在一种新的体内抗癌中空纤维试验中进行进一步测试。

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