期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 14, 页码 4965-4974出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.06.013
关键词
Claisen-Schmidt reaction; Pyrazolic chalcones; Functionalized dihydropyrazoles; Cyclocondensation reaction; Antitumoral agents; Microwave irradiation
资金
- Colciencias
- Universidad del Valle
- Consejeria de Innovacion
- Ciencia y Empresa (Junta de Andalucia, Spain)
- Universidad de Jaen
Novel (E)-1-aryl-3-(3-aryl-1-phenyl-1H-pyrazol-4-yl)prop-2-en-1-ones 5/6 (pyrazolic chalcones) were synthesized from a Claisen-Schmidt reaction of 3-aryl-1-phenylpyrazol-4-carboxaldehydes 4 with several acetophenone derivatives 1. Subsequently, the microwave-assisted cyclocondensation reaction of chalcones 5/6 with hydrazine afforded the new racemic 3-aryl-4-(3-aryl-4,5-dihydro-1H-pyrazol-5-yl)-1-phenyl-1H-pyrazoles 7 or their N-acetyl derivatives 8 and 9 when reactions where carried out in DMF or acetic acid, respectively. Several of these compounds were screened by the US National Cancer Institute (NCI) for their ability to inhibit 60 different human tumor cell lines, where 5c and 9g showed remarkable activity mainly against leukemia (K-562 and SR), renal cancer (UO-31) and non-small cell lung cancer (HOP-92) cell lines, with the most important GI(50) values ranging from 0.04 to 11.4 mu M, from the in vitro assays. (C) 2010 Elsevier Ltd. All rights reserved.
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