Bandarage Upul K, Wang Tiansheng, Come Jon H, Perola Emanuele, Wei Yunyi, Rao B Govinda
Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, MA 02139, USA.
Bioorg Med Chem Lett. 2008 Jan 1;18(1):44-8. doi: 10.1016/j.bmcl.2007.11.014. Epub 2007 Nov 13.
A series of potent thiol-containing aryl sulfone TACE inhibitors were designed and synthesized. The SAR and MMP selectivity of the series were investigated. In particular, compound 8b showed excellent in vitro potency against the isolated enzyme and good selectivity over MMP-2, -7, -8, -9, and -13. The X-ray structure of 8b in complex with TACE was also obtained.
设计并合成了一系列含硫醇的强效芳基砜TACE抑制剂。研究了该系列化合物的构效关系（SAR）和基质金属蛋白酶（MMP）选择性。特别地，化合物8b对分离酶显示出优异的体外活性，并且对MMP-2、-7、-8、-9和-13具有良好的选择性。还获得了8b与TACE复合物的X射线晶体结构。
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