Benzothiazole-containing hydroxamic acids as histone deacetylase inhibitors and antitumor agents
- Authors
- Dao Thi Kim Oanh; Hoang Van Hai; Park, Sang Ho; Kim, Hyun-Jung; Han, Byung-Woo; Kim, Hyung-Sook; Hong, Jin-Tae; Han, Sang-Bae; Van Thi My Hue; Nguyen-Hai Nam
- Issue Date
- Dec-2011
- Publisher
- PERGAMON-ELSEVIER SCIENCE LTD
- Keywords
- Histone deacetylase (HDAC) inhibitors; Benzothiazole; Heterocycle
- Citation
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.21, no.24, pp 7509 - 7512
- Pages
- 4
- Journal Title
- BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Volume
- 21
- Number
- 24
- Start Page
- 7509
- End Page
- 7512
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/21035
- DOI
- 10.1016/j.bmcl.2011.07.124
- ISSN
- 0960-894X
1464-3405
- Abstract
- Data from clinical studies indicate that inhibitors of Class I and Class II histone deacetylase (HDAC) enzymes show great promise for the treatment of cancer. Zolinza (SAHA, Zolinza) was recently approved by the FDA for the treatment of the cutaneous manifestations of cutaneous T-cell lymphoma. As a part of our ongoing effort to identify novel small molecules to target these important enzymes, we have prepared two series of benzothiazole-containing analogues of SAHA. It was found that several compounds with 6C-bridge linking benzothiazole moiety and hydroxamic functional groups showed good inhibition against HDAC3 and 4 at as low as 1 mu g/ml and exhibited potent cytotoxicity against five cancer cell lines with average IC50 values of as low as 0.81 mu g/ml, almost equipotent to SAHA. (C) 2011 Published by Elsevier Ltd.
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Collections - College of Pharmacy > School of Pharmacy > 1. Journal Articles
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