Bristol-Myers Squibb Research, PO Box 4000, Princeton, NJ 08543, USA.
Bioorg Med Chem Lett. 2012 Jun 15;22(12):3946-50. doi: 10.1016/j.bmcl.2012.04.103. Epub 2012 May 2.
A series of phenylacylsulfonamides has been prepared as antagonists of Bcl-2/Bcl-xL. In addition to potent binding affinities for both Bcl-2 and Bcl-xL, these compounds were shown to induce classical markers of apoptosis in isolated mitochondria. Overall weak cellular potency was improved by the incorporation of polar functionality resulting in compounds with moderate antiproliferative activity.
已经制备了一系列苯甲酰基磺酰胺作为 Bcl-2/Bcl-xL 的拮抗剂。这些化合物不仅对 Bcl-2 和 Bcl-xL 具有很强的结合亲和力，还能在分离的线粒体中诱导典型的凋亡标志物。通过引入极性官能团，整体上提高了细胞活性较弱的化合物的细胞活性，得到了具有中等抗增殖活性的化合物。
