Organosilicon compounds as adult T-cell leukemia cell proliferation inhibitors

Masaharu Nakamura, Yotaro Matsumoto, Masaaki Toyama, Masanori Baba, Yuichi Hashimoto

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)

Abstract

Aggressive forms of adult T-cell leukemia (ATL) respond poorly to conventional anticancer chemotherapy, and new lead compounds are required for the development of drugs to treat this fatal disease. Recently, we developed ATL cell-selective proliferation inhibitors based on a tetrahydrotetramethylnaphthalene (TMN) skeleton 1, and here we report the design and synthesis of silicon analogs of TMN derivatives. Among them, compound 13 showed the most potent growth-inhibitory activity towards the ATL cell line S1T, though its selectivity for S1T over the non-ATL cell line MOLT-4 was only moderate. This result, as well as computational studies, suggests that sila-substitution (C/Si exchange) is useful for structure optimization of these inhibitors.

Original languageEnglish
Pages (from-to)237-241
Number of pages5
JournalChemical and Pharmaceutical Bulletin
Volume61
Issue number2
DOIs
Publication statusPublished - 2013 Feb

Keywords

  • Adult T-cell leukemia
  • Sila-substitution
  • Silicon
  • T-lymphotropic virus type 1
  • Tetrahydrotetramethylnaphthalene skeleton

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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