Pyrrolo[2,1-c][1,2,4]triazines from 2-diazopyrroles: synthesis and antiproliferative activity |
| |
Authors: | Diana Patrizia Barraja Paola Lauria Antonino Montalbano Alessandra Almerico Anna Maria Dattolo Gaetano Cirrincione Girolamo |
| |
Institution: | Dipartimento Farmacochimico Tossicologico e Biologico dell'Università, Via Archirafi 32, 90123 Palermo, Italy. |
| |
Abstract: | Pyrrolo2,1-c]1,2,4]triazines 4a-g were directly obtained from the reaction of 2-diazopyrroles 1a and b with the sodium salts of beta-diketones, beta-carbonitriles, and beta-dinitriles. Only when the 2-diazopyrroles were coupled with ethyl cyanoacetate, it was possible to isolate, together with the pyrrolotriazines, the intermediate hydrazones 3 which, in turn, cyclised to the title ring system. Pyrrolotriazines 4a-e were evaluated for cytotoxic activity against a panel of 60 human cancer cell lines by the National Cancer Institute and some of them demonstrated inhibitory effects in the growth of a wide range of cancer cell lines generally at 10(-5) M level and in some cases at micromolar concentrations. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|