不含过渡金属的C–N和C–C的形成:由炔酮合成苯并[4,5]咪唑并[1,2- a ]吡啶和2-吡啶酮
摘要:
在此,已经揭示了在温和条件下炔烃与2-甲基苯并咪唑的无过渡金属的有效级联反应。该级联反应涉及迈克尔加成/分子内环加成/脱水,并以中等至良好的产率提供了所需的苯并[4,5]咪唑并[1,2- a ]吡啶。此外,三种苯并[4,5]咪唑并[1,2- a ]吡啶(3d,3i和3q)对Hep-G2(人类肝癌),T-24(人类膀胱癌细胞)和SK-OV-3(人类卵巢癌)细胞系,IC 50值在8.05–10.67μmolL -1范围内。为了研究有效抑制细胞生长的机制,对细胞周期分析,凋亡率检测,Ca 2+生成的测量,ROS,线粒体膜电位测定和caspase-3 / 9活化进行了进一步的研究。化合物3i。
COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS
申请人:Kossen Karl
公开号:US20090318455A1
公开(公告)日:2009-12-24
Disclosed are compounds and methods for treating inflammatory and fibrotic disorders, including methods of modulating a stress activated protein kinase (SAPK) system with an active compound, wherein the active compound exhibits low potency for inhibition of the p38 MAPK; and wherein the contacting is conducted at a SAPK-modulating concentration that is at a low percentage inhibitory concentration for inhibition of the p38 MAPK by the compound. Also disclosed are derivatives and analogs of pirfenidone, useful for modulating a stress activated protein kinase (SAPK) system.
Katrizky, Alan R.; Oniciu, Daniela C.; Mancheno, Balbino, Journal of the Chemical Society. Perkin transactions I, 1994, # 1, p. 113 - 119
作者:Katrizky, Alan R.、Oniciu, Daniela C.、Mancheno, Balbino、Barcolk, Richard A.
DOI:——
日期:——
Katritzky Alan R., Oniciu Daniela C., Mancheno Balbino, Barcock Richard A+, J. Chem. Soc. Perkin Trans. 1, (1994) N 1, S 113-118
作者:Katritzky Alan R., Oniciu Daniela C., Mancheno Balbino, Barcock Richard A+
DOI:——
日期:——
METHODS FOR TREATING ACUTE MYOCARDIAL INFARCTIONS AND ASSOCIATED DISORDERS
申请人:Olgin Jeff
公开号:US20100190731A1
公开(公告)日:2010-07-29
The invention relates to methods of treating patients who have suffered an acute myocardial infarction (AMI) with a therapeutic that has anti-fibrotic effects, for example, pirfenidone and analogs thereof.
Methods for Treating Acute Myocardial Infarctions and Associated Disorders
申请人:Olgin Jeff
公开号:US20110218515A1
公开(公告)日:2011-09-08
The invention relates to methods of treating patients who have suffered an acute myocardial infarction (AMI) with a therapeutic that has anti-fibrotic effects, for example, pirfenidone and analogs thereof.