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Yao Xue Xue Bao ; 48(9): 1430-5, 2013 Sep.
Article in Chinese | MEDLINE | ID: mdl-24358777

ABSTRACT

Dihydroartemisinin is an important derivative of artemisinin. We used dihydroartemisinin as the starting material, through esterification, amination and acylation, a series of novel piperazine-sulfonamide contained dihydroartemisinin derivatives were firstly synthesized and their chemical structures were confirmed by IR, 1H NMR, 13C NMR and HR-MS. X-diffraction was used to determine the final configuration of the compound 3c. And the in vitro anti-HeLa activities of compounds 3 were analyzed with CCK-8 method. The preliminary bioassay test shows that compound 3 showed the best inhibition activities against HeLa with IC50 values of 0.14 micromol x L(-1).


Subject(s)
Antineoplastic Agents/chemical synthesis , Artemisinins/chemical synthesis , Cell Proliferation/drug effects , Piperazines/chemical synthesis , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Artemisinins/chemistry , Artemisinins/pharmacology , HeLa Cells , Humans , Inhibitory Concentration 50 , Molecular Structure , Piperazine , Piperazines/chemistry , Piperazines/pharmacology , Structure-Activity Relationship , Sulfonamides/chemistry
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