Halogenated benzimidazole carboxamides target integrin α 4β1 on T-cell and B-cell lymphomas

Richard D. Carpenter, Arutselvan Natarajan, Edmond Y Lau, Mirela Andrei, Danielle M. Solano, Felice C Lightstone, Sally J. DeNardo, Kit Lam, Mark J. Kurth

Research output: Contribution to journalArticlepeer-review

14 Scopus citations


Integrin α4β1 is an attractive but poorly understood target for selective diagnosis and treatment of T-cell and B-cell lymphomas. This report focuses on the rapid microwave preparation, structure-activity relationships, and biological evaluation of medicinally pertinent benzimidazole heterocycles as integrin α4β 1 antagonists. We documented tumor uptake of derivatives labeled with 125I in xenograft murine models of B-cell lymphoma. Molecular homology models of integrin α4β1 predicted that docked halobenzimidazole carboxamides have the halogen atom in a suitable orientation for halogen-hydrogen bonding. The high-affinity halogenated ligands identified offer attractive tools for medicinal and biological use, including fluoro and iodo derivatives with potential radiodiagnostic (18F) or radiotherapeutic (131I) applications, or chloro and bromo analogues that could provide structural insights into integrin-ligand interactions through photoaffinity, cross-linking/mass spectroscopy, and X-ray crystallographic studies.

Original languageEnglish (US)
Pages (from-to)5448-5456
Number of pages9
JournalCancer Research
Issue number13
StatePublished - Jul 1 2010

ASJC Scopus subject areas

  • Cancer Research
  • Oncology


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