title: Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'.
abstract: STAT3 is a promising molecular target for the design of new anticancer drugs. In this paper, we report the design and synthesis of a conformationally constrained macrocyclic peptidomimetic 2 via click chemistry. Compound 2 was determined to bind to STAT3 with a K(i) value of 7.3 microM in a competitive fluorescence-polarization-based binding assay, representing a promising initial lead compound for further optimization.
authors.affiliation: University of Michigan Comprehensive Cancer Center, Department of Internal Medicine, University of Michigan, Ann Arbor, MI 48109, USA.
authors.forename: Jianyong
authors.initials: J
authors.lastname: Chen
authors.forename: Zaneta
authors.initials: Z
authors.lastname: Nikolovska-Coleska
authors.forename: Chao-Yie
authors.initials: CY
authors.lastname: Yang
authors.forename: Cindy
authors.initials: C
authors.lastname: Gomez
authors.forename: Wei
authors.initials: W
authors.lastname: Gao
authors.forename: Krzysztof
authors.initials: K
authors.lastname: Krajewski
authors.forename: Sheng
authors.initials: S
authors.lastname: Jiang
authors.forename: Peter
authors.initials: P
authors.lastname: Roller
authors.forename: Shaomeng
authors.initials: S
authors.lastname: Wang
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D005454:Fluorescence Polarization; D008958:Models, Molecular; D008968:Molecular Conformation; D050796:STAT3 Transcription Factor / Q000037:antagonists & inhibitors*
chemical_list: D000970:Antineoplastic Agents; D050796:STAT3 Transcription Factor