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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:28

Article

Mathew, Bini¹  Snowden, Timothy S.²  Connelly, Michele C.³  Guy, R. Kiplin⁴  Reynolds, Robert C.⁵ 

[1] Southern Res Inst, Drug Discovery Div, 2000 Ninth Ave South, Birmingham, AL 35205 USA

[2] Univ Alabama, Dept Chem & Biochem, 250 Hackberry Lane, Tuscaloosa, AL 35487 USA

[3] St Jude Childrens Res Hosp, Dept Chem Biol & Therapeut, 262 Danny Thomas Pl,Mailstop 1000, Memphis, TN 38105 USA

[4] Univ Kentucky, Coll Pharm, 214H BioPharm Complex, Lexington, KY 40536 USA

[5] Univ Alabama Birmingham, Div Hematol & Oncol, Birmingham, AL 35294 USA

关键词: Sulindac;    Profens;    Chemoprevention;    Anticancer;    Chemical biology;   

DOI  :  10.1016/j.bmcl.2018.05.023

来源: Elsevier

【 摘 要 】

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 alpha-methyl substituted sulindac amides in the profen class. Several compounds of this series displayed promising activity compared with a lead sulindac analog.

【 授权许可】

Free