Amino acid derivatives as histone deacetylase inhibitors

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• 作者：Jed L. Hubbs ; Hua Zhou ; Astrid M. Kral ; Judith C. Fleming ; William K. Dahlberg ; Bethany L. Hughes ; Richard E. Middleton ; Alex ; er A. Szewczak ; J. Paul Secrist ; Thomas A. Miller
• 关键词：Histone deacetylase ; Cancer ; Ugi reaction ; Lysine ; Amino acid ; Benzothiophene
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 出版时间：1 January 2008
• 年：2008
• 卷：18
• 期：1
• 页码：34-38
• 全文大小：129 K

文摘

Ongoing 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 an ongoing effort to identify novel small molecules to target these important enzymes, we have prepared several classes of amino acid-derived HDAC1 inhibitors. The design rationale and in vitro activity against the HDAC1 enzyme and HCT116 cell line are described in this letter.