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Antitumor agents 281. Design, synthesis, and biological activity of substituted 4-amino-7,8,9,10-tetrahydro-2H-benzo[h]chromen-2-one analogs (ATBO) as potent in vitro anticancer agents.

Abstract
In our exploration of new biologically active chemical entities, we designed and synthesized a novel class of antitumor agents, substituted 4-amino-7,8,9,10-tetrahydro-2H-benzo[h]chromen-2-one (ATBO) analogs. We evaluated their cytotoxic activity against seven human tumor cell lines from different tissues, and established preliminary structure-activity relationships (SAR). All analogs, except 8, 9, and 25-27, displayed potent tumor cell growth inhibitory activity. Especially, compounds 15 and 33 with a 4-methoxyphenyl group at position C-4 were extremely potent with ED(50) values of 0.008-0.064 and 0.035-0.32 μM, respectively. Compound 15 was the most potent analog compared with structurally related neo-tanshinlactone (e.g., 1) and 4-amino-2H-benzo[h]chromen-2-one (ABO, e.g., 4) analogs, and thus merits further exploration as an anti-cancer drug candidate.
AuthorsYizhou Dong, Kyoko Nakagawa-Goto, Chin-Yu Lai, Susan L Morris-Natschke, Kenneth F Bastow, Kuo-Hsiung Lee
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 21 Issue 1 Pg. 546-9 (Jan 01 2011) ISSN: 1464-3405 [Electronic] England
PMID21087859 (Publication Type: Journal Article, Research Support, N.I.H., Extramural)
CopyrightCopyright © 2010 Elsevier Ltd. All rights reserved.
Chemical References
  • 4-((4'-methoxyphenyl)amino)-7,8,9,10-tetrahydro-2H-benzo(h)chromen-2-one
  • Aniline Compounds
  • Antineoplastic Agents
  • Chromones
  • Coumarins
Topics
  • Aniline Compounds (chemical synthesis, chemistry, therapeutic use)
  • Antineoplastic Agents (chemical synthesis, chemistry, therapeutic use)
  • Cell Line, Tumor
  • Chromones (chemical synthesis, chemistry, therapeutic use)
  • Coumarins (chemical synthesis, chemistry, therapeutic use)
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Humans
  • Neoplasms (drug therapy)
  • Structure-Activity Relationship

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