Design and practice of phenobarbital comprehensive experiment / 中华医学教育探索杂志

A set of comprehensive chemical experiments was designed for the second-year undergraduate majoring in pharmacy which contained synthesis,refinement,structural identification and appraisal analysis and assaying in phenobarbital.The purpose of the experiment was to improve the comprehensive strength,the ability of investigation and operation.The paper mainly discusses the design and application of the comprehensive experiment in the phenobarbital for pharmacy and Chinese medicine majors from the following aspects including design idea,teaching plan,effectiveness and popularization.

Synthesis and JAK2 inhibitory activities of 4-phenyl-pyrrolo[2, 3-d] pyrimidine derivatives / 中国药科大学学报

A series of 4-phenyl-pyrrolo[2,3-d] pyrimidine derivatives were synthesized through modifying the structure of the lead compound ruxolitinib by molecular hybridization strategy.It was synthesized from pyrimidine-4,6-diol by Vilsmeier-Haack reaction,SNAr reaction,cyclized,dehydration,Suzuki coupling and finally acylated to give 12 new compounds(12a-121).All structures of the synthesized compounds were confirmed by 1H NMR,13C NMR,and HRMS analysis.The biological activities were evaluated in vitro.Their JAK2 inhibitory activities were studied using JAK2 enzymatic and TF1-GMCSF cellular assays.The results indicated that compounds 12b,12e and 12h showed moderate activity.The anti-tumor activities were studied against JAK2-independent A549 cell line by the MTT assay.Results showed that the tide compounds exhibited potent antiproliferative effect on A549,especially compound 12c(IC50 =0.12 μmol/L),suggesting that this series compounds might be promising anti-tumor agents for futher investigation.

Design, synthesis and bioactivities of 4-(3-sulfonylbenzene) amino-6-formylpyrrole2,3-d pyrimidine derivatives / 中国药科大学学报

Taking JAK2 inhibitor baricitinib and fedratinib as the lead compounds,to design the novel 4-(3-sulfonylbenzene) amino-6-formylpyrrole[2,3-d] pyrimidine JAK2 inhibitors nucleus using the molecular hybrid drug design principle.17 target compounds were synthesized by derivatization of sulfonyl and formyl groups respectively.We used JAK2 kinase and GM-CSF-induced TF-1 cells to measure the activities of compounds.The results showed that most compounds had JAK2 inhibitory activities.Among them,compound 31 had excellent inhibitory activity on JAK2 kinase (IC50 =0.009 μmol/L) and GM-CSF-induced TF-1 cells (IC50 =0.136 μmol/L),which proved that the compound had potential research and development value.