4.5 Article

Design, synthesis and insight into the structure-activity relationship of 1,3-disubstituted indazoles as novel HIF-1 inhibitors

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 21, Pages 6297-6300

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.08.120

Keywords

YC-1; HIF-1 alpha; SAR (structure-activity relationship); Hypoxia; Anti-cancer agent

Funding

  1. National Research Foundation of Korea (NRF)
  2. Korean Government (MEST) [20100028431]
  3. Research Institute of Pharmaceutical Science, Seoul National University

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Design, synthesis and insight into the structure-activity relationship (SAR) of 1,3-disubstituted indazoles as novel HIF-1 inhibitors are described. In particular, the substituted furan moiety on indazole skeleton as well as its substitution pattern turns out crucial for the high HIF-1 inhibition. (C) 2011 Elsevier Ltd. All rights reserved.

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