Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'

Bioorganic and Medicinal Chemistry Letters

Volumn 17, Issue 14, 2007, Pages 3939-3942

  Chen, Jianyong ^a   Nikolovska Coleska, Zaneta ^a   Yang, Chao Yie ^a   Gomez, Cindy ^a   Gao, Wei ^a   Krajewski, Krzysztof ^b   Jiang, Sheng ^b   Roller, Peter ^b   Wang, Shaomeng ^a  

^a UNIVERSITY OF MICHIGAN COMPREHENSIVE CANCER CENTER   (United States)

^b NATIONAL CANCER INSTITUTE   (United States)

Author keywords

Click chemistry; Conformationally; Constrained mimetic; STAT3

Indexed keywords

ANTINEOPLASTIC AGENT; MACROCYCLIC COMPOUND; PROTEIN INHIBITOR; STAT3 PROTEIN; STAT3 PROTEIN INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; BINDING ASSAY; CHEMISTRY; CLICK CHEMISTRY; DRUG CONFORMATION; DRUG DESIGN; DRUG MECHANISM; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; FLUORESCENCE POLARIZATION; STRUCTURE ANALYSIS;

ANTINEOPLASTIC AGENTS; DRUG DESIGN; FLUORESCENCE POLARIZATION; MODELS, MOLECULAR; MOLECULAR CONFORMATION; STAT3 TRANSCRIPTION FACTOR;

EID: 34250349898     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.04.096     Document Type: Article

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12. 6) δ ppm 8.55 (d, J = 9.0 Hz, 1H), 7.89 (d, J = 9.4 Hz, 1H), 7.51 (s, 1H), 6.49 (d, J = 7.8 Hz, 1H), 4.87-4.80 (m, 1H), 4.32-4.09 (m, 4H), 3.72-3.69 (m, 1H), 3.67 (s, 3H), 3.20-3.15 (m, 1H), 3.01-2.92 (m, 1H), 1.80-1.30 (m, 4H), 1.35 (s, 9H), 1.01 (s, 9H), 1.02 (d, J = 6.0 Hz, 3H), 0.92-0.60 (m, 2H).
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