Design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as STAT3 inhibitors.
The STAT3 oncogene is a promising molecular target for the design of a new class of anticancer drugs. In this letter, we describe the design, synthesis, and evaluation of peptidomimetics containing Freidinger lactams as novel STAT3 inhibitors. Compound 3 binds to STAT3 with a K(i) value of 190nM and is a promising lead compound for further design and optimization.
Gomez
Cindy
C
Cancer Center, University of Michigan, Ann Arbor, MI 48109, USA.
Bai
Longchuan
L
Zhang
Jian
J
Nikolovska-Coleska
Zaneta
Z
Chen
Jianyong
J
Yi
Han
H
Wang
Shaomeng
S
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D032701:Biomimetics; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007700:Kinetics; D007769:Lactams / Q000138:chemical synthesis* / Q000494:pharmacology; D008956:Models, Chemical; D015394:Molecular Structure; D010748:Phosphopeptides / Q000737:chemistry; D010766:Phosphorylation; D011487:Protein Conformation; D050796:STAT3 Transcription Factor / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D007769:Lactams; D010748:Phosphopeptides; D050796:STAT3 Transcription Factor