title: Design and synthesis of a biotinylated probe of COX-2 inhibitor nimesulide analog JCC76.
abstract: JCC76 is a derivative of cyclooxygenase-2(COX-2) selective inhibitor nimesulide and exhibits potent anti-breast cancer activity. It selectively induces apoptosis of Her2 positive breast cancer cells. However, the specific molecular targets of JCC76 still remain unclear, which significantly withdraw the further drug development of JCC76. To identify the molecular targets of JCC76, a six carbon linker and biotin conjugated JCC76 probe was designed and synthesized. The anti-proliferation activity of the probe and its analogs was evaluated.
authors.affiliation: Department of Chemistry, College of Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
authors.forename: Bo
authors.initials: B
authors.lastname: Zhong
authors.forename: Rati
authors.initials: R
authors.lastname: Lama
authors.forename: Kerri M
authors.initials: KM
authors.lastname: Smith
authors.forename: Yan
authors.initials: Y
authors.lastname: Xu
authors.forename: Bin
authors.initials: B
authors.lastname: Su
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D015374:Biosensing Techniques; D019921:Biotinylation; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D060326:Chemistry Techniques, Synthetic; D003509:Cyclohexanecarboxylic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015394:Molecular Structure; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D003509:Cyclohexanecarboxylic Acids; D052246:Cyclooxygenase 2 Inhibitors; D013449:Sulfonamides; C560272:cyclohexanecarboxylic acid (3-(2,5-dimethylbenzyloxy)-4-(methanesulfonylmethylamino)phenyl)amide