"Click" synthesis of small-molecule inhibitors targeting caspases.
A panel of 198 P4-diversified aldehyde (reversible) and vinyl sulfone (irreversible) inhibitors is successfully synthesized via an efficient "click chemistry" platform and directly screened against caspase-3 and -7 for inhibition.
Ng
Su Ling
SL
Department of Chemistry, National University of Singapore, 3 Science Drive 3, Singapore 117543.
Yang
Peng-Yu
PY
Chen
Kitty Y-T
KY
Srinivasan
Rajavel
R
Yao
Shao Q
SQ
D000447:Aldehydes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D061945:Caspase Inhibitors; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D008968:Molecular Conformation; D008970:Molecular Weight; D054852:Small Molecule Libraries / Q000138:chemical synthesis*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013450:Sulfones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D000447:Aldehydes; D061945:Caspase Inhibitors; D004791:Enzyme Inhibitors; D054852:Small Molecule Libraries; D013450:Sulfones; C009873:divinyl sulfone