用于探究抗癌构效关系的舒林酸α-甲基酰胺类似物的小型多样性文库。
A small diversity library of α-methyl amide analogs of sulindac for probing anticancer structure-activity relationships.
作者信息
Mathew Bini, Snowden Timothy S, Connelly Michele C, Guy R Kiplin, Reynolds Robert C
机构信息
Drug Discovery Division, Southern Research Institute, 2000 Ninth Avenue South, Birmingham, AL 35205, USA.
Department of Chemistry and Biochemistry, The University of Alabama, 250 Hackberry Lane, Tuscaloosa, AL 35487, USA.
出版信息
Bioorg Med Chem Lett. 2018 Jul 1;28(12):2136-2142. doi: 10.1016/j.bmcl.2018.05.023. Epub 2018 May 10.
Non-steroidal anti-inflammatory drugs (NSAIDs) have a variety of potential indications that include management of pain and inflammation as well as chemoprevention and/or treatment of cancer. Furthermore, a specific form of ibuprofen, dexibuprofen or the S-(+) form, shows interesting neurological activities and has been proposed for the treatment of Alzheimer's disease. In a continuation of our work probing the anticancer activity of small sulindac libraries, we have prepared and screened a small diversity library of α-methyl substituted sulindac amides in the profen class. Several compounds of this series displayed promising activity compared with a lead sulindac analog.
非甾体抗炎药（NSAIDs）有多种潜在适应症，包括疼痛和炎症的管理以及癌症的化学预防和/或治疗。此外，布洛芬的一种特定形式，右布洛芬或S-(+)形式，显示出有趣的神经学活性，并已被提议用于治疗阿尔茨海默病。在我们探索小的舒林酸文库抗癌活性工作的延续中，我们制备并筛选了一个小的α-甲基取代舒林酸酰胺类的多样文库，属于丙酸类。与一种先导舒林酸类似物相比，该系列的几种化合物显示出有前景的活性。
Zotero 插件