YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
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Parameter Focusing on the Topoisomerase I-inhibition Activities of 1-(2-furyl)-3-phenylpropenone Derivatives

1-(2-furyl)-3-phenylpropenone 유도체의 DNA Topoisomerase I 저해활성에 대한 parameter focusing

  • 명평근 (충남대학교 약학대학 약학과) ;
  • 최수라 (충남대학교 약학대학 약학과) ;
  • 성낙도 (충남대학교 농과대학 응용생물화학부)
  • Published : 2000.08.01
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Abstract

Parameter focusing on the DNA topoisomerase-Iinhibition with X-substituted phenyl substituents in 1-(2-furyl)-3-phenylpropenone derivatives as inhibition material were analyzed. From the basis on the results the inhibition on DNA topoisomerase I suggested that the inhibition activities of X-substituted phenyl substitutents would depend largely on the net charge of $\beta$-carbon atom, LUMO energy (e.v.) and STERIMOL parameter B$_{5}$ (width) of X. Among them, non-substituent (X=H), 1 and 2,2-dichloro substituent, 4 showed the highest DNA topoisomerase-I inhibition activity.y.

Keywords

References

  1. Kor. J. Agri. Chem. v.42 Inhibition of farnesyl transferase inhibition activity of chalcone derivatives Myung, P.K.;Sung, N.D.;Yu, S.J.;Kwon, B.M.;Lee, S.H.
  2. Kor. J. Pestic. Sci. v.2 Influence of substituted phenyl backborn of the fungicidal activity of 2-thienyl and 2-furyl substituents in bis-aromatic alpha, α, β-unsaturated ketone derivatives Myung, P.K.;Sung, N.D.;Yu, S.J.;Kwon, B.M.;Lee, S.H.
  3. Argi. Chem. Biotech. v.37 Fungicidal activity of 3-(X-sub.phenyl)-1-(2-furyl) propenone derivatives Sung, N.D.;Kang, H.D.;Maeng, J.Y.;Shin, D.R.
  4. Kor. J. Agri. Chem. v.42 The cytotoxicity of 1,3-diphenylpropene derivatives Sung, N.D.;Yu, S.J.;Choi, S.U.;Kwon, B.M.;Lee, C.D.
  5. 日本特許出願公開番號, 6-122623 紫田承二;求田信草;岩田進;西野剛史;抗腫瘍濟
  6. Cancer. Chemoth v.50 Experimental screening procedures and clinicals predictably value Goldin, A.;Serpick, A.A.;Mantel, N.
  7. Yakhak Hoeji v.44 Antimatherogenic effects of curcumin in hypercholesterolemic rabbits Kim, T.G.;Kim, H.E.;Kang, S.Y.;Jung, K.K.;Park, Y.B.;Choi, M.S.;Lee, H.S.;Han, H.M.
  8. Med. Res. Rev. v.17 Recent advances in the discovery and development of topoisomerase inhibitors as antitumor agents Wang, H.K.;Morris-Natschke, L.S.;Lee, K.H.
  9. IUPAC Pesticide Chemistry, human welfare and the environment v.Ⅰ Magee, P.S.
  10. Yakhak Hoeji v.44 6-(1-hydroxy or acyloxyallkyl(-5,8-dialkoxy-1,4-naphthoquinones:synthesis, evaluation of cytotoxic activity, antitumor activity and inhibitory effect on DNA Topoisomerase-Ⅰ. Kim, Y.;Choi, S.L.;Myung, P.K.;Ahn, B.Z.
  11. CLOGP Program (Ver. 3.53) LogP, Calculation algorithm
  12. Hyperchem (Ver. 4.0) Hyperchem. for windows Chemical calculation
  13. Org. Magn. Reson. v.8 Investigation of substituent effects of chalcones by C NMR Spectroscopy Solaniova. E.;Toma. S.;Gronowitz, S.
  14. ACS professional reference book Exploring QSAR fundamental and applications in chemistry and biology Hansch, C.;Leo A.
  15. Kor. Soc. Agri. Chem. & Biotech. v.43 parameter focusing on the topoisomerase Ⅰ inhibition activities of 6-(1-acyloxyalkyl)-5,8-dialkoxy-1,4-naphthoquinone derivatives Sung, N.D.;Myung, P.K.