Title of article :
Modification of cap group in δ-lactam-based histone deacetylase (HDAC) inhibitors
Author/Authors :
Hwan-Mook Kim، نويسنده , , Sung Hee Hong، نويسنده , , Myung Sook Kim، نويسنده , , Chang Woo Lee، نويسنده , , Jong Soon Kang، نويسنده , , Kiho Lee، نويسنده , , Song Kyu Park، نويسنده , , Jeung Whan Han، نويسنده , , Hee-Yoon Lee، نويسنده , , Yongseok Choi، نويسنده , , Ho Jeung Kwon، نويسنده , , Gyoonhee Han، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2007
Pages :
5
From page :
6234
To page :
6238
Abstract :
Novel δ-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.
Keywords :
Anticancer chemotherapy , Enzyme inhibitor , In vivo xenograft model , Docking model , growth inhibition , Histone deacetylase , HDAC
Journal title :
Bioorganic & Medicinal Chemistry Letters
Serial Year :
2007
Journal title :
Bioorganic & Medicinal Chemistry Letters
Record number :
798782
Link To Document :
بازگشت