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KMID : 0903519990420030252
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Journal of the Korean Society of Agricultural Chemistry and Biotechnology
1999 Volume.42 No. 3 p.252 ~ p.255
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The Farnesyl Protein Transferase Inhibition Activity of Chalcone Derivatives
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이승호/Lee, Seung Ho
성낙도/유성재/명평근/권병목/Sung, Nack Do/Yu, Seong Jae/Myung, Pyung Keun/Kwon, Byung Mok
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Abstract
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Inhibition activities(pI_(50)) of chalcone derivatives as substrate with farnesyl protein transferase(FPTase) were determined in vitro. The structure activity relationships(SAR) between the activity and physicochemical parameters of X & Y-substituents on the phenyl groups were analyzed by Free-Wilson and Hansch method. X-substituents on the benzoyl group have the more important role to inhibition activity than Y-substituents on the styryl group. Among them, none substituent, 8 showed the highest FPTase inhibition activity(pI_(50)=4.30). Particularly, the SAR equation could be formulated, showing a parabolic relationship between the activity and hydrophobicity(logP) where the optimal value(∑logP)_(opt) was 3.915. And also the activity depends on the steric effect(Es$gt;0) with X-substituent and the resonance effect(R$lt;0) with electron donating Y-substituents. Based on the results of SAR analyses, the interactions between substrates and receptor, FPTase, could be assumed.
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KEYWORD
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