以20(S)-喜树碱(6)为原料,经氧化,光反应重排,制得10-羟基喜树碱(4)并对其工艺条件进行了改进,氧化产率由60.2%提高到86.1%,光反应产率由30.6%提高到49.8%;再以10-羟基喜树碱(4)为原料,经乙酰化、Minisci自由基反应、水解反应,最终得到2...以20(S)-喜树碱(6)为原料,经氧化,光反应重排,制得10-羟基喜树碱(4)并对其工艺条件进行了改进,氧化产率由60.2%提高到86.1%,光反应产率由30.6%提高到49.8%;再以10-羟基喜树碱(4)为原料,经乙酰化、Minisci自由基反应、水解反应,最终得到20(S)-7-对氟苯甲酰基-10-羟基喜树碱(1),并用IR、1 H NMR和MS进行了结构表征。用SRB法对1进行了体外抗肿瘤活性实验,显示1对人白血病(HL-60)、人胃癌细胞(BCG-823)、人肝癌细胞(Bel-7402)和人鼻咽癌细胞(KB)均有抑制作用。展开更多
The binding reactions between topotecan hydrochloride(THC) or 10-hydroxycamptothecin(HCPT) and transferrin bovine(Tf) are studied by fluorescence and UV-Vis absorption spectra.The research results indicate that the co...The binding reactions between topotecan hydrochloride(THC) or 10-hydroxycamptothecin(HCPT) and transferrin bovine(Tf) are studied by fluorescence and UV-Vis absorption spectra.The research results indicate that the combination reaction of them is a single static quenching process,camptothecin derivatives strongly bound Tf with the molar ratio of 1∶1,the equilibrium constant(K0) at 25 oC are as follows,K0(THC)=2.38×105L·mol-1,K0(HCPT) =2.43×106 L·mol-1.The shortest binding distance(r)between donor(Tf) and acceptor(camptothecin derivatives) are obtained by Frster’s nonradiative energy transfer mechanism,rTHC =3.77nm,rHCPT =3.92.The enthalpy change(△H) and entropy change(△S) are calculated at 25 oC and 37 oC,the results indicate that hydrophobic interaction and the diple-diple force play a major role in the binding of camptothecin derivatives and Tf.The results of 1H NMR spectrum show that the active groups of HCPT interacting with Tf are 10-OH.展开更多
文摘以20(S)-喜树碱(6)为原料,经氧化,光反应重排,制得10-羟基喜树碱(4)并对其工艺条件进行了改进,氧化产率由60.2%提高到86.1%,光反应产率由30.6%提高到49.8%;再以10-羟基喜树碱(4)为原料,经乙酰化、Minisci自由基反应、水解反应,最终得到20(S)-7-对氟苯甲酰基-10-羟基喜树碱(1),并用IR、1 H NMR和MS进行了结构表征。用SRB法对1进行了体外抗肿瘤活性实验,显示1对人白血病(HL-60)、人胃癌细胞(BCG-823)、人肝癌细胞(Bel-7402)和人鼻咽癌细胞(KB)均有抑制作用。
文摘The binding reactions between topotecan hydrochloride(THC) or 10-hydroxycamptothecin(HCPT) and transferrin bovine(Tf) are studied by fluorescence and UV-Vis absorption spectra.The research results indicate that the combination reaction of them is a single static quenching process,camptothecin derivatives strongly bound Tf with the molar ratio of 1∶1,the equilibrium constant(K0) at 25 oC are as follows,K0(THC)=2.38×105L·mol-1,K0(HCPT) =2.43×106 L·mol-1.The shortest binding distance(r)between donor(Tf) and acceptor(camptothecin derivatives) are obtained by Frster’s nonradiative energy transfer mechanism,rTHC =3.77nm,rHCPT =3.92.The enthalpy change(△H) and entropy change(△S) are calculated at 25 oC and 37 oC,the results indicate that hydrophobic interaction and the diple-diple force play a major role in the binding of camptothecin derivatives and Tf.The results of 1H NMR spectrum show that the active groups of HCPT interacting with Tf are 10-OH.
