新型螺异恶唑啉类抗癌剂的合成与研究
Synthesis and Investigation of Novel Spiro-isoxazolines as Anti-Cancer Agents.
作者信息
Das Prasanta, Omollo Ann O, Sitole Lungile J, McClendon Eric, Valente Edward J, Raucher Drazen, Walker Leslie R, Hamme Ashton T
机构信息
Department of Chemistry & Biochemistry, Jackson State University 1400 J. R. Lynch St, PO Box 17910, Jackson, Ms 39217, USA.
Department of Chemistry, University of Portland, Portland, OR 97203, USA.
出版信息
Tetrahedron Lett. 2015 Apr 1;56(14):1794-1797. doi: 10.1016/j.tetlet.2015.02.059.
A series of structurally diverse 4-bromo spiro-isoxazolines possessing a variety of aromatic and aliphatic substituents at the 3 position, were synthesized through a 1,3-dipolar cycloaddition followed by intramolecular cyclization of a pendant hydroxyl or carboxylic acid group. The biochemical antiproliferative activity was evaluated by using two breast cancer cell lines (MCF-7 and MDA-MB-231) and two prostate cancer cell lines (PC-3 and DU-145) using the MTT viability assay, and the IC values were obtained. Spiro-isoxazoline derivatives bearing a -chloro or an -dichloro aromatic substituent at the 3-position of the isoxazoline showed considerable antitumor activities in all four cell lines with IC value ranging from 43μM to 56μM.
通过1,3 - 偶极环加成反应，随后使侧链羟基或羧酸基团进行分子内环化，合成了一系列结构多样的4 - 溴螺异恶唑啉，其在3位具有各种芳族和脂族取代基。使用MTT活力测定法，通过两种乳腺癌细胞系（MCF - 7和MDA - MB - 231）和两种前列腺癌细胞系（PC - 3和DU - 145）评估了生化抗增殖活性，并获得了IC值。在异恶唑啉的3位带有氯或二氯芳族取代基的螺异恶唑啉衍生物在所有四种细胞系中均显示出相当大的抗肿瘤活性，IC值范围为43μM至56μM。
Zotero 插件