RESUMEN
A series of 4-(N-aryl)amino-6-alkoxyl pteridine derivatives was designed and synthesized via the bio-isostere principle using anti-cancer drugs with quinazoline cores as lead compounds.The proliferative inhibitory activities of the synthesized compounds against tumor cells A549,KG1a and HGC-27 were also performed by MTT assay.Using methyl 3-aminopyrazine-2-carboxylate as the starting material,12 target compounds(7a-7l)were synthesized through six-step reaction, and characterized by 1H NMR, 13C NMR and MS.It was showed that antitumor activity of pteridines with 2-chloro-5-nitro-anilino substituted in position 4 was more potent than that of others.The activity of compound 7b on A549 cells(IC50=11.55 μmol/L)was closely approximate to that of positive control gefitinib(IC50=5.95 μmol/L).IC50values of compound 7k on three cell lines were all close to those of gefitinib.A 2-chloro-5-nitro-anilino fragment was contained in preferred compounds which might be modified for further investigation.
RESUMEN
Objective: To synthesize new desired 5-chlorobenzotriazole derivatives by ultrasonic-microwave radiation and perform structural characterization. Methods:5-Chlorobenzotriazole was used as the starting material and reacted with chloroacetonitrile to obtain the intermediate product, and then respectively reacted with 6-chloro nicotinaldehyde and 5-formaldehude-2-methoxy-pyridine to obtain corresponding target compounds. Results: Six desired 5-chlorobenzotriazole compounds have been synthesized and their structures were confirmed by melting point, IR, LC-MS and 1 H-NMR. Conclusion:Six desired 5-chlorobenzotriazole compounds are synthesized by ul-trasonic-microwave radiation.
RESUMEN
Objective To study the method which was used to prepare naproxen microcapsule with alginate-chitosan by means of a complex coacervation method in an emulsion system.MethodsThe orthogonal experimental design using the standard of drug encapsulation was applied to optimize the preparation procedure of the microcapsules.Results The optimal preparation condition was as follows: r=500r?min-1,pH=4.0,C(chitosan)=3%,T=50℃.Conclusion This method was reproducible,and the results of the experiment in vitro indicated that the microcapsule obtained under these conditions may sustained release of drugs.