A small diversity library of α-methyl amide analogs of sulindac for probing anticancer structure-activity relationships

构建了一个包含舒林酸α-甲基酰胺类似物的小型多样性化合物库,用于探索抗癌化合物的构效关系。

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Abstract

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.

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