Abstract:
:Small molecules that act on multiple biological targets have been proposed to combat the drug resistance commonly observed for cancer chemotherapy. By combining the structural features of known inhibitors of inosine monophosphate dehydrogense (IMPDH) and histone deacetylase (HDAC), dual inhibitors of IMPDH and HDAC based on the scaffold of cinnamic hydroxamic acid (CHA) have been designed, synthesized, and evaluated in biological assays. Key features, including the linker length, linker functionality, substitution position, and interacting groups, have been explored. Their individual contribution to the inhibitory activities against human IMPDH1 and IMPDH2 as well as HDAC has been assessed.
journal_name
Bioorg Med Chemjournal_title
Bioorganic & medicinal chemistryauthors
Chen L,Petrelli R,Gao G,Wilson DJ,McLean GT,Jayaram HN,Sham YY,Pankiewicz KWdoi
10.1016/j.bmc.2010.06.081subject
Has Abstractpub_date
2010-08-15 00:00:00pages
5950-64issue
16eissn
0968-0896issn
1464-3391pii
S0968-0896(10)00609-7journal_volume
18pub_type
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