Parallel synthesis and biocatalytic amplification of a cross-conjugated cyclopentenone library.
A combination of parallel chemical synthesis and biocatalysis has been used to prepare and amplify a library of cross-conjugated cyclopentenones. A number of marine and terrestrial natural products with antibiotic activity are known to incorporate this pharmacophore. The library was screened for anticancer, antimycobacterial, antifungal, and antibacterial activity. The positive results from the screens provide an indication of the structural features that are associated with activity in the various assays and suggest promising avenues for further inquiry.
Jang
W B
WB
Department of Chemistry, 2545 The Mall, University of Hawaii, Honolulu, Hawaii 96822, USA.
Hu
H
H
Lieberman
M M
MM
Morgan
J A
JA
Stergiades
I A
IA
Clark
D S
DS
Tius
M A
MA
D001711:Biotransformation; D020650:Combinatorial Chemistry Techniques; D003517:Cyclopentanes / Q000138:chemical synthesis*; D010450:Endopeptidases / Q000737:chemistry; D004798:Enzymes / Q000737:chemistry*; D007202:Indicators and Reagents; D008049:Lipase / Q000737:chemistry; D010084:Oxidation-Reduction; D010544:Peroxidases / Q000378:metabolism; D012441:Saccharomyces cerevisiae / Q000378:metabolism; D013025:Glycine max / Q000201:enzymology
D003517:Cyclopentanes; D004798:Enzymes; D007202:Indicators and Reagents; D010544:Peroxidases; D008049:Lipase; D010450:Endopeptidases; C013905:cyclopentenone