Abstract:
:A small library of boron-cluster- and metallacarborane-cluster-based ligands was designed, prepared, and tested for isoform-selective activation or inhibition of the three nitric oxide synthase isoforms. On the basis of the concept of creating a hydrophobic analogue of a natural substrate, a stable and nontoxic basic boron cluster system, previously used for boron neutron capture therapy, was modified by the addition of positively charged moieties to its periphery, providing hydrophobic and nonclassical hydrogen bonding interactions with the protein. Several of these compounds show efficacy for inhibition of NO synthesis with differential effects on the various nitric oxide synthase isoforms.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Kaplánek R,Martásek P,Grüner B,Panda S,Rak J,Masters BS,Král V,Roman LJdoi
10.1021/jm300805xsubject
Has Abstractpub_date
2012-11-26 00:00:00pages
9541-8issue
22eissn
0022-2623issn
1520-4804journal_volume
55pub_type
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