期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 14, 页码 3939-3942出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.04.096
关键词
STAT3; conformationally; constrained mimetic; click chemistry
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, value of 7.3 mu M in a competitive fluorescence-polarization-based binding assay, representing a promising initial lead compound for further optimization. (C) 2007 Elsevier Ltd. All rights reserved.
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