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KMID : 0903519990420010068
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Journal of the Korean Society of Agricultural Chemistry and Biotechnology
1999 Volume.42 No. 1 p.68 ~ p.72
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The Cytotoxicity of l,3-diphenylpropenone derivatives
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이정옥/Lee, Chong Ock
최상운/성낙도/유성재/권병목/Choi, sang Un/Sung, Nack Do/Yu, Seong Jae/Kwon, Byung Mok
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Abstract
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The cytotoxicity of 1,3-diphenylpropenone derivatives known to inhibit the famesyl protein transferase (FPTase) was examined against various established tumor cell line, A549 (lung cancer), SKMEL-2 (uterine cancer), HCT-15 (skin cancer), SKOV-3 (brain cancer) and XF-498 (colon cancer) of the 1,3-diphenylpropenone derivatives showing farnesyl protein transferase (FPTase) inhibition activity. And the structure-activity relationship (SAR) between structure of 1,3-diphenylpropenone derivatives as substrate and cytotoxicity was investigated by Free-Wilson analysis as well as Hansch method with tumor cell lines. From the result of Free-Wilson analyses, X-substituents on the benzoyl group have a more important role than Y-substituents on the styryl group. The 2,4-dichloro substituent, 15 and 2,4-dimethyl substituent, 16 showed the highest cytotoxicity (average pI_(50)=5.0). Particulary, the cytotoxicity of X-substituents increased with electronic effect (σ) due to weak electron withdrawing group with optimum value (σ_(opt)=0.22∼0.29) whereas that of Y-substituent resulted from various factors such as logP, B₁ and R constant.
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KEYWORD
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