Department of Chemistry, Saurashtra University, Rajkot 360005, India.
Eur J Med Chem. 2011 May;46(5):1942-8. doi: 10.1016/j.ejmech.2011.02.045. Epub 2011 Feb 23.
A new series of benzofuran-2-yl(4,5-diydro-3,5-substituted diphenylpyrazol-1-yl) methanone derivatives 8a-x by the reaction of the benzofuran-2-carbohydrazides 7 with various chalcone derivatives 3a-x using microwave irradiation has been described. The effect of synthesized compounds 8a-v was studied against human cancer cell lines for their antiproliferative activity and reversal of multidrug resistance on human MDR1-gene transfected mouse lymphoma cells. Among the 24 compounds, the 8c and 8h showed good antiproliferative activity 8b, 8f and 8k were exhibited good MDR reversal activity. The main significance of the process is easy workup process, short reaction time and high yield of the new compounds for biological interest. However, the studies on genetically modified multidrug resistant cancer cells are costly and time consuming.
通过用微波辐射使苯并呋喃-2-甲酰肼 7 与各种查尔酮衍生物 3a-x 反应，合成了一系列新的苯并呋喃-2-基（4,5-二氢-3,5-取代二苯基吡唑-1-基）甲酮衍生物 8a-x。研究了合成化合物 8a-v 对人癌细胞系的抗增殖活性和对人 MDR1 基因转染的小鼠淋巴瘤细胞的多药耐药性的逆转作用。在 24 种化合物中，8c 和 8h 表现出良好的抗增殖活性，8b、8f 和 8k 表现出良好的多药耐药性逆转活性。该方法的主要优点是操作简单、反应时间短、新化合物产率高，具有生物研究意义。然而，对遗传修饰的多药耐药性癌细胞的研究既昂贵又耗时。
