N-(7-吲唑基)苯磺酰胺衍生物作为有效的细胞周期抑制剂的合成及生物学评价
Synthesis and biological evaluation of N-(7-indazolyl)benzenesulfonamide derivatives as potent cell cycle inhibitors.
作者信息
Bouissane L, El Kazzouli S, Léonce S, Pfeiffer B, Rakib E M, Khouili M, Guillaumet G
机构信息
Institut de Chimie Organique et Analytique, UMR CNRS 6005, Université d'Orléans, BP 6759, France.
出版信息
Bioorg Med Chem. 2006 Feb 15;14(4):1078-88. doi: 10.1016/j.bmc.2005.09.037. Epub 2005 Nov 7.
PMID:16274996
Abstract
We herein describe a new synthesis of N-(7-indazolyl)benzenesulfonamide derivatives. These compounds were evaluated for their antiproliferative activities toward L1210 murine leukemia cells. One of them, 4-methoxy-N-(3-chloro-7-indazolyl)benzenesulfonamide, was identified as the most potent with an IC(50) of 0.44 microM.
摘要
我们在此描述了一种新型的N-(7-吲唑基)苯磺酰胺衍生物的合成方法。对这些化合物针对L1210小鼠白血病细胞的抗增殖活性进行了评估。其中之一，4-甲氧基-N-(3-氯-7-吲唑基)苯磺酰胺，被确定为活性最强的，其半数抑制浓度（IC50）为0.44微摩尔。
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