Uecker, Andrea and Sicker, Marit and Beckers, Thomas and Mahboobi, Siavosh and Hagerstrand, Daniel and Ostman, Arne and Boehmer, Frank-D. (2010) Chimeric tyrosine kinase-HDAC inhibitors as antiproliferative agents. ANTI-CANCER DRUGS, 21 (8). pp. 759-765. ISSN 0959-4973,
Full text not available from this repository. (Request a copy)Abstract
Combined treatment with tyrosine kinase inhibitors (TKi) and additional drugs is emerging as a promising strategy for cancer therapy. TKi and histone-deacetylase inhibitors (HDI) are two classes of anti-tumor agents with distant mechanisms of action. We have designed and synthesized chimeric compounds, which comprise structural elements of the TKi imatinib, and of prototypical HDI compounds. These compounds retain TKi activity similar to imatinib, exemplified by the inhibition of the platelet-derived growth factor receptor, and c-Kit kinase in intact cells. In addition, the chimeric compounds have in vitro and cellular HDI activity, and potently inhibit growth of cancer cell lines, including that of imatinib-resistant cell lines. Chimeric molecules with combined TKi and HDI activity may simplify combination treatment and be applicable to overcome clinical resistance to TKi single-agent therapy. Anti-Cancer Drugs 21: 759-765 (C) 2010 Wolters Kluwer Health vertical bar Lippincott Williams & Wilkins.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | HISTONE DEACETYLASE INHIBITORS; GROWTH-FACTOR RECEPTOR; MYELOGENOUS LEUKEMIA; POTENT INHIBITORS; ANTICANCER AGENTS; MYELOID-LEUKEMIA; CANCER-THERAPY; IMATINIB; APOPTOSIS; CELLS; chimeric compound; HDAC inhibitor; imatinib; PDGF receptor; tyrosine kinase inhibitor |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry I (Prof. Elz) |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 13 Jul 2020 09:36 |
| Last Modified: | 13 Jul 2020 09:36 |
| URI: | https://pred.uni-regensburg.de/id/eprint/24200 |
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