摘要
通过NMR及粘度测定,本文研究了7个具有不同取代基的萘并噻吩系列化合物与DNA结合的方式。认定无论取代基的电性如何,此系列化合物均以嵌插络合的方式与DNA结合。通过光谱及热力学测量,比较了取代基的电性效应对本系列化合物与DNA结合强度的影响,发现Hammett取代基常数σ与小分子—DNA络合物的表观稳定常数K(LogK)值有一定的相关性,并据此初步探讨了其反应机制。
An investigation of structure-activity relationship between 6-substituted naphtho-thiophenes andDNA has been made. All compounds bind to DNA by intercalation based on increases in viscosity ofDNA and upfield ~1H NMR chemical shifts with DNA. The spectroscopic and calorimetric measurementsshow both electron withdrawing and donating groups at position 6 increase the binding constant (K).The well-defined biphasic correlation between Hammett substituent constant (σ) and logK for bindingand the change in slope of a Hammett plot have been interpreted as a change in mechanism of theintetaction between small molecule and DNA.
出处
《北京医科大学学报》
CSCD
1991年第4期325-328,共4页
Journal of Peking University(Health Sciences)
关键词
脱氧核糖核酸
萘并噻吩
取代基常数
Deoxyribonucleic acid
Naphtho-thiophene
Intercalation
Hammett substituent constant
