Synthesis and biological evaluation of novel FK228 analogues as potential isoform selective HDAC inhibitors
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- 作者：Koichi Naritaa ; Keisuke Matsuharaa ; Jun Itoha ; Yui Akiyamaa ; Singo Danb ; Takao Yamorib ; c ; Akihiro Itod ; Minoru Yoshidad ; Tadashi Katoha ; katoh@tohoku-mpu.ac.jp" class="auth_mail" title="E-mail the corresponding author
- 关键词：FK228 analogues ; Histone deacetylase inhibitors ; Structure-activity relationship ; Bicyclic depsipeptide ; Total synthesis
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：4 October 2016
- 年：2016
- 卷：121
- 期：Complete
- 页码：592-609
- 全文大小：835 K
文摘
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Eight new FK228 analogues were synthesized.
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These analogues were evaluated against HDACs and 39 human cancer cell lines.
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Some of these analogues exhibited very high HDAC1 (class I) isoform selectivity.
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Potent and highly isoform-selective HDAC1 inhibitors were identified.
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Novel aspects of SAR were revealed.