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KMID : 0903519980410040218
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Journal of the Korean Society of Agricultural Chemistry and Biotechnology
1998 Volume.41 No. 4 p.218 ~ p.221
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Inhibition of Farnesyl Protein Transferase by Ortho - substituted Cinnamaldehyde Derivatives
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Kwon, Byoung Mog
Cho, Young Kwon/Sung, Nack Do/Lim, Chi Hwan
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Abstract
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Various cinnamaldehyde derivatives were synthesized and their inhibition activity (pI_(50)) of farnesyl protein transferase (FPTase) was measured to examine the structure-activity relationships (SAR) on the basis that FPTase was inhibited by ortho-hydroxycinnamaldehyde derived from extracts of the bark of Cinnamomum cassia Blume. The ortho-substituents on the phenyl backbone of cinnamaldehyde showed higher activity than those with meta- and para-substituents, and the side chain required unsaturated aldehyde. In particular, 2-chlorocinnamaldehyde, 5 showed the highest inhibition activity on the FPTase among them and its inhibition activity (pI_(50)) value was 4.45.
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