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抗癌剂。IV. 某些新型1-氮杂咔唑衍生物作为抗肿瘤剂的合成

Cancerostatics. IV. On the synthesis of some noval 1-Azacarbazole derivatives as antineoplastic agents.

作者信息

Kaczmarek L, Nantka-Namirski P

出版信息

Pol J Pharmacol Pharm. 1981 Jan-Feb;33(1):121-7.

PMID:7255278
Abstract

By condensation of 2-chloro-3-nitropyridine with some anilines the corresponding 2-anilino-3-nitropyridines 1a--11 were obtained. Hydrogenation of these compounds and subsequent diazotization of the 2-anilino-3-aminopyridine derivatives 2a--2l gave triazoles 3a--3l which thermally decomposed in PPA or in liquid paraffine afforded the required 6- and 8-substituted 1-azacarbazole derivatives 4a--3, i--l. Some of these compounds showed significant activity against transplanted mouse sarcoma 180. None of them were active against L 1210 and P 388 leukemias.

摘要

通过使2-氯-3-硝基吡啶与一些苯胺缩合,得到了相应的2-苯胺基-3-硝基吡啶1a - 11。这些化合物经氢化以及随后对2-苯胺基-3-氨基吡啶衍生物2a - 2l进行重氮化反应,得到三唑3a - 3l,其在多聚磷酸(PPA)或液体石蜡中热分解,得到所需的6-和8-取代的1-氮杂咔唑衍生物4a - 3、i - l。其中一些化合物对移植的小鼠肉瘤180显示出显著活性。它们对L 1210和P 388白血病均无活性。

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