A novel class of highly potent multidrug resistance reversal agents: Disubstituted adamantyl derivatives

Kyung Hoon Min, Yan Xia, Eun Kyung Kim, Yinglan Jin, Navneet Kaur, Eun Seon Kim, Dae Kyong Kim, Hwa Young Jung, Yongseok Choi, Mi Kyung Park, Yong Ki Min, Kiho Lee, Kyeong Lee

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

Novel disubstituted adamantyl derivatives were synthesized and evaluated in a P-glycoprotein dependent multidrug resistance cancer cell line. The hit to lead optimization provided potent MDR reversal agents. Some potent adamantyl derivatives were more than 10-fold more potent than verapamil without considerable intrinsic cytotoxicity. The 3-trifluorophenyl derivative 14f did not affect the metabolism of CYP450 3A4, whereas most of MDR revertants had a weak inhibitory effect.

Original languageEnglish
Pages (from-to)5376-5379
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume19
Issue number18
DOIs
Publication statusPublished - 2009 Sep 15

Keywords

  • ABC transporter
  • Adamantane
  • CYP3A4
  • MES-SA/DX5
  • Multidrug resistance
  • P-glycoprotein

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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  • Cite this

    Min, K. H., Xia, Y., Kim, E. K., Jin, Y., Kaur, N., Kim, E. S., Kim, D. K., Jung, H. Y., Choi, Y., Park, M. K., Min, Y. K., Lee, K., & Lee, K. (2009). A novel class of highly potent multidrug resistance reversal agents: Disubstituted adamantyl derivatives. Bioorganic and Medicinal Chemistry Letters, 19(18), 5376-5379. https://doi.org/10.1016/j.bmcl.2009.07.127