Menarini Ricerche, Via Tito Speri 10, 00040 Pomezia, Rome, Italy.
Bioorg Med Chem Lett. 2013 Jul 15;23(14):4091-5. doi: 10.1016/j.bmcl.2013.05.053. Epub 2013 May 25.
In the search for a new class of histone deacetylase inhibitors, we prepared a series of simple benzofused hydroxamic acids to find an anchoring fragment of minimal molecular weight. These initial hits, all belonging to the benzothiophene class, showed very good ligand efficiencies. Following these findings, a classical fragment growing approach was performed to increase binding affinity and cytotoxicity.
在寻找新型组蛋白去乙酰化酶抑制剂的过程中，我们合成了一系列简单的苯并稠合羟肟酸，以寻找最小分子量的锚定片段。这些最初的命中化合物均属于苯并噻吩类，表现出非常好的配体效率。基于这些发现，我们采用了经典的片段生长方法来提高结合亲和力和细胞毒性。
