Synthesis and antitumor activity of α-aminophosphonate derivatives containing thieno[2,3-d]pyrimidines

Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive α-aminophosphonate subunits were introduced at the N3 position through an N-N bond connection. The in vitro cytotoxic activity of the novel compounds was tested against human esophageal carcinoma cells （EC109）, human hepatocarcinoma cells （HepG2）, human gastric carcinoma cells （MGC-803）, respectively, by the MTT method. The evaluation results revealed that compounds fimb, 6mf, 6mg, 6rid and 6nh exerted the most potent inhibition against HepG2, MGC-803 and EC109 cells, respectively. In particular, compound 6rag presented excellent inhibitory effect against HepG2 （91.2%） and MGC-803 （94.4%） cells.

Synthesis and structure-activity relationships study ofα-aminophosphonate derivatives containing a quinoline moiety

Two series of a-aminophosphonate derivatives containing a quinoline moiety have been designed and synthesized by introducing bioactive quinoline scaffold to a-aminophosphonate. The in vitro cytotoxic activities of target compounds were first investigated against two human cancer cell lines including Eca109 and Huh7 by MTT assay. Results revealed that most of target compounds exhibited moderate to high antitumor activities against the tested cancer cell lines and some demonstrated more potent inhibitory activities compared with Sunitinib. Among them, compounds 4b2 and 4b4 containing methylsubstituted aniline group were found to be more active than Sunitinib against both of two cancer cell lines, with IC50 in the range of 2.26 mmol/L–7.46 mmol/L.

Novel pyrazole fused heterocyclic ligands:Synthesis,characterization,DNA binding/cleavage activity and anti-BVDV activity

A series of novel pyrazole fused heterocyclic derivatives were synthesized via a two-step procedure or a one-pot two step method, and their catalytic DNA cleavage abilities and anti-BVDV activities were also evaluated. The results obtained indicated that compounds 3b-3c could catalyze the cleavage of supercoiled DNA （pUC 19 plasmid DNA） to nicked DNA under physiological conditions with high yields via a hydrolytic mechanism. The studies on anti-viral activities against bovine viral diarrhea virus （BVDV） demonstrated that some of the pyrazole derivatives showed pronounced anti-BVDV activity with interesting ECso values and no significant cytotoxicity. Among them, compound 31 showed the highest antiviral activity （ECso = 0.12 μmol/L） and was 10 fold more than that of the positive control ribavirin （ECso = 1.3 μmol/L）, which provided a potential candidate for the development of anti-BVDV agents.

30 cases of popliteal cyst treated by fire needling and cupping therapy

Objective:To explore the therapeutic effect of the fire needling with the three-edged needle and the cupping on popliteal cyst.Methods:A total of 60 patients of popliteal cyst were divided into two groups,30 cases in each one according to the random number table.In the fire needling group,the burnt-red three-edged needle was inserted to the deep layer of the cyst.After the fluid was squeezed out,the cupping was exerted.The treatment was given 1 to 2 times a week,for 4 weeks totally.In the western medication group,prednisolone acetate 25 mg was injected in the cyst capsule,once a week,for 4 weeks totally.The effective rate,recurrence rate and Rauschning-Lindgren grading were evaluated before and after treatment.Results:The total effective rate was 80.0%in the fire needling group and was 83.3%in the western medication group,without statistical significance in comparison(P>0.05).The recurrence rate was 6.7%in the fire needling group and was 30%in the western medication group.The recurrence rate in the fire needling group was lower than that in the western medication group,indicating the statistical significance(P<0.05).After treatment,Rauschning-Lindgren grade was different statistically as compared with that before treatment in either group(both P<0.05).Rauschning-Lindgren grade was distributed in 0 to I in the fire needling group after treatment,which was different significantly as compared with the western medication group(P<0.05).Conclusion:The combined treatment with the fire needling combined with cupping therapy achieves the satisfactory effect on popliteal cyst and the very low recurrence rate and it is easy in operation and deserves to be promoted in primary care.