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Synthesis and cytotoxic evaluation of novel spirohydantoin derivatives of the dihydrothieno[2,3-b]naphtho-4,9-dione system.

Abstract
The synthesis and cytotoxic evaluation of 3-(alkyl)(alkyl-substituted)spiro[(dihydroimidazo-2,4-dione)-5,3'-(2',3'-dihydrothieno[2,3-b]naphtho-4',9'-dione)]derivatives are described. Evaluation of these analogues against the MCF-7 human breast carcinoma and SW 620 human colon carcinoma cell lines uncovered for most of the compounds a cytotoxic potency comparable to or greater than that of doxorubicin. Compound 15 exhibited remarkable cytotoxic activity against several other human solid tumor cell lines. Interestingly, only a partial cross-resistance to compound 15 in selected tumor cell sublines known to be resistant to doxorubicin (MCF-7/Dx and A2780/Dx) was observed, whereas a total absence of cross-resistance in a tumor cell subline selected for resistance to cisplatin was found (A2780/DDP).
AuthorsIsabel Gomez-Monterrey, Giovanni Santelli, Pietro Campiglia, Daniela Califano, Fabiano Falasconi, Claudio Pisano, Loredana Vesci, Teresa Lama, Paolo Grieco, Ettore Novellino
JournalJournal of medicinal chemistry (J Med Chem) Vol. 48 Issue 4 Pg. 1152-7 (Feb 24 2005) ISSN: 0022-2623 [Print] United States
PMID15715481 (Publication Type: Journal Article)
Chemical References
  • 3-(3-(N,N-dimethyl)aminopropyl)spiro((dihydroimidazo-2,4-dione)-5,3'-(2',3'-dihydrothieno(2,3-b)naphtho-4',9'-dione))
  • Antineoplastic Agents
  • Hydantoins
  • Naphthoquinones
  • Spiro Compounds
  • Topoisomerase II Inhibitors
  • Doxorubicin
  • Cisplatin
Topics
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Cell Line, Tumor
  • Cisplatin (pharmacology)
  • Doxorubicin (pharmacology)
  • Drug Resistance, Neoplasm
  • Drug Screening Assays, Antitumor
  • Humans
  • Hydantoins (chemical synthesis, chemistry, pharmacology)
  • Molecular Conformation
  • Naphthoquinones (chemical synthesis, chemistry, pharmacology)
  • Spiro Compounds (chemical synthesis, chemistry, pharmacology)
  • Stereoisomerism
  • Structure-Activity Relationship
  • Topoisomerase II Inhibitors

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