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

Parameter Focusing on the Topoisomerase I-inhibition Activities of 1-(2-furyl)-3-phenylpropenone Derivatives

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Parameter focusing on the DNA topoisomerase-I inhibition 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, B5 (width) of X. Among them, non-substituent (X=H), 1 and 2,2-dichloro substituent, 4 showed the highest DNA topoisomerase-I inhibition activity.

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