Benzo[b]tellurophenes as a potential histone H3 lysine 9 demethylase (KDM4) inhibitor

Yoon Jung Kim, Dong Hoon Lee, Yong Sung Choi, Jin Hyun Jeong, So Hee Kwon

Research output: Contribution to journalArticle

Abstract

Gene expression and tumor growth can be regulated by methylation levels of lysine residues on histones, which are controlled by histone lysine demethylases (KDMs). Series of benzo[b]tellurophene and benzo[b]selenophene compounds were designed and synthesized and they were evaluated for histone H3 lysine 9 demethylase (KDM4) inhibitory activity. Among the carbamates, alcohol and aromatic derivatives, tert-butyl benzo[b]tellurophen-2-ylmethylcarbamate (compound 1c) revealed KDM4 specific inhibitory activity in cervical cancer HeLa cells, whereas the corresponding selenium or oxygen substitute compounds did not display any inhibitory activity toward KDM4. Compound 1c also induced cell death in cervical and colon cancer but not in normal cells. Thus, compound 1c, a novel inhibitor of KDM4, constitutes a potential therapeutic and research tool against cancer.

Original languageEnglish
Article number5908
JournalInternational journal of molecular sciences
Volume20
Issue number23
DOIs
Publication statusPublished - 2019 Dec 1

Bibliographical note

Funding Information:
Funding: This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education (NRF-2016R1A6A3A11932164, NRF-2017R1A6A3A11034603, 2018R1A6A1A03023718, and 2019R1A2C1008619).

All Science Journal Classification (ASJC) codes

  • Catalysis
  • Molecular Biology
  • Spectroscopy
  • Computer Science Applications
  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Inorganic Chemistry

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