van Rensburg Michelle, Leung Euphemia, Haverkate Natalie A, Eurtivong Chatchakorn, Pilkington Lisa I, Reynisson Jóhannes, Barker David
School of Chemical Sciences, University of Auckland, New Zealand.
Auckland Cancer Society Research Centre and Department of Molecular Medicine and Pathology, University of Auckland, New Zealand.
Bioorg Med Chem Lett. 2017 Jan 15;27(2):135-138. doi: 10.1016/j.bmcl.2016.12.009. Epub 2016 Dec 5.
3-Amino-2-arylcarboxamide-thieno[2,3-b]pyridines are a known class of antiproliferative compounds with activity against the phospholipase C enzyme. To further investigate the structure activity relationships of these derivatives a series of analogues were prepared modifying key functional groups. It was determined that modification of the 3-amino and 2-aryl carboxamide functionalities resulted in complete elimination of activity, whilst modification at C-5 allowed compounds of greater activity to be prepared.
3-氨基-2-芳基甲酰胺基噻吩并[2,3-b]吡啶是一类已知的具有抗磷脂酶C酶活性的抗增殖化合物。为了进一步研究这些衍生物的构效关系,制备了一系列修饰关键官能团的类似物。结果表明,3-氨基和2-芳基甲酰胺官能团的修饰导致活性完全丧失,而在C-5位的修饰则使得能够制备出活性更高的化合物。