Applied Biological Chemistry
- Volume 42 Issue 1
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- Pages.68-72
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- 1999
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- 2468-0834(pISSN)
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- 2468-0842(eISSN)
The Cytotoxicity of 1,3-diphenylpropenone derivatives
1,3-diphenylpropenone 유도체의 세포독성
- Yu, Seong-Jae (Division of Applied Biology & Chemistry, Chung-nam National University) ;
- Kwon, Byung-Mok (Protein Regulator R.U., Korea Research Institute Bioscience and Biotechnology) ;
- Lee, Chong-Ock (Screening and Toxicology Research Center, Korea Research Insititute of Chemical Technology) ;
- Choi, Sang-Un (Screening and Toxicology Research Center, Korea Research Insititute of Chemical Technology) ;
- Sung, Nack-Do (Division of Applied Biology & Chemistry, Chung-nam National University)
- 유성재 (충남대학교 농과대학 응용생물화학부) ;
- 권병목 (생명공학연구소, 단백질 조절 연구부) ;
- 이정옥 (한국화학연구소 스크리닝 연구부) ;
- 최상운 (한국화학연구소 스크리닝 연구부) ;
- 성낙도 (충남대학교 농과대학 응용생물화학부)
- Published : 1999.02.28
Abstract
The cytotoxicity of 1,3-diphenylpropenone derivatives known to inhibit the farnesyl 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
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