2. Academic Validation
  3. Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors

Modification of cap group in delta-lactam-based histone deacetylase (HDAC) inhibitors

  • Bioorg Med Chem Lett. 2007 Nov 15;17(22):6234-8. doi: 10.1016/j.bmcl.2007.09.034.
Hwan Mook Kim 1,  Sung Hee Hong,  Myung Sook Kim,  Chang Woo Lee,  Jong Soon Kang,  Kiho Lee,  Song-Kyu Park,  Jeung Whan Han,  Hee Yoon Lee,  Yongseok Choi,  Ho Jeung Kwon,  Gyoonhee Han
Affiliations

Affiliation

  • 1 Korea Research Institute of Bioscience and Biotechnology, Yuseong, Daejeon 305-333, Republic of Korea.
PMID: 17904843 DOI: 10.1016/j.bmcl.2007.09.034
Abstract

Novel delta-lactam-based HDAC inhibitors which have various substituted benzyl, bi-aromatic cap groups were prepared using ring closure metathesis reaction, and evaluated their HDAC inhibitory activities and anti-proliferative effects. Among prepared analogues, 11m and 11o have very strong HDAC enzymatic inhibition and showed the most potent growth inhibitory activity to five human tumor cell lines including PC-3, ACHN, NUGC-3, HCT-15, and MBA-MB-231 tumor cell lines. Compounds 11m and 11o also showed good tumor growth inhibition of MDA-MB-231 cells in in vivo xenograft model. Structure-activity relationship study using docking model explained the significance of hydrophobic aromatic cap groups for their in vitro activities.

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