التفاصيل البيبلوغرافية
| العنوان: |
Data from Halogenated Benzimidazole Carboxamides Target Integrin α4β1 on T-Cell and B-Cell Lymphomas |
| المؤلفون: |
Mark J. Kurth, Kit S. Lam, Sally J. DeNardo, Felice C. Lightstone, Danielle M. Solano, Mirela Andrei, Edmond Y. Lau, Arutselvan Natarajan, Richard D. Carpenter |
| بيانات النشر: |
American Association for Cancer Research (AACR), 2023. |
| سنة النشر: |
2023 |
| الوصف: |
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 α4β1 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. Cancer Res; 70(13); 5448–56. ©2010 AACR. |
| URL الوصول: |
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::664072d35f8e6155e4f60d85bccb4ae2
https://doi.org/10.1158/0008-5472.c.6500661 |
| حقوق: |
OPEN |
| رقم الأكسشن: |
edsair.doi.dedup.....664072d35f8e6155e4f60d85bccb4ae2 |
| قاعدة البيانات: |
OpenAIRE |
