Monastrol analogs: A synthesis of pyrazolopyridine, benzopyranopyrazolopyridine, and oxygen-bridged azolopyrimidine derivatives and their biological screening

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:20

Article

Svetlik, Jan¹  Veizerova, Lucia¹  Mayer, Thomas U.²  Catarinella, Mario² 

[1] Comenius Univ, Dept Pharmaceut Anal & Nucl Pharm, SK-83232 Bratislava, Slovakia

[2] Univ Konstanz, Dept Mol Genet, D-78457 Constance, Germany

关键词: Biginelli reaction;    Hantzsch reaction;    Oxygen-bridged nitrogen heterocycles;    Monastrol analogs;   

DOI  :  10.1016/j.bmcl.2010.05.085

来源: Elsevier

【 摘 要 】

A synthesis of novel pyrazolopyridine, benzopyranopyrazolopyridine, and oxygen-bridged pyrazolo-, tetrazolo, benzimidazo-, and thiazolopyrimidines via Hantzsch- and Biginelli-like condensations has been developed. The ability of these compounds to inhibit Eg5 activity has been examined. The results indicate that synthetic manipulations in the monastrol thiourea moiety are inefficient. (C) 2010 Elsevier Ltd. All rights reserved.

【 授权许可】

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