Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: Effects on HDAC biology and antiproliferative activity |
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| Authors: | Subhasish Tapadar Rong He Doris N. Luchini Daniel D. Billadeau Alan P. Kozikowski |
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| Affiliation: | 1. Department of Medicinal Chemistry & Pharmacognosy, University of Illinois at Chicago, 833 South Wood Street Chicago, IL 60612, USA;2. Division of Oncology Research, College of Medicine, Mayo Clinic, Rochester, MN 55905, USA |
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| Abstract: | A series of hydroxamic acid based histone deacetylase inhibitors 6–15, containing an isoxazole moiety adjacent to the Zn-chelating hydroxamic acid, is reported herein. Some of these compounds showed nanomolar activity in the HDAC isoform inhibitory assay and exhibited micro molar inhibitory activity against five pancreatic cancer cell lines. |
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