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Synthesis and in vitro antimalarial activity of tetraoxane-amine/amide conjugates |
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| Authors: | Kumar Nitin Khan Shabana I Atheaya Himanshu Mamgain Ritu Rawat Diwan S |
| Affiliation: | a Department of Chemistry, University of Delhi, Delhi 110007, India b National Centre for Natural Products Research, School of Pharmacy, University of Mississippi, MS 38677, USA c Department of Pharmacognosy, School of Pharmacy, University of Mississippi, MS 38677, USA |
| Abstract: | A series of tetraoxanes, tetraoxane-amine and tetraoxane-amide conjugates have been synthesized and screened for in vitro antimalarial activity against chloroquine-sensitive and chloroquine-resistant strains of Plasmodium falciparum. Most of the conjugates showed slightly better antimalarial activity than the parent tetraoxanes. Three of the conjugate compounds were potentially active with IC50 values in the range of 0.38-0.80 μM. Cytotoxicity of four selected compounds was also evaluated in a panel of four cancer (SK-MEL, KB, BT-549, SK-OV-3) and two non-cancer (Vero and LLC-PK11) cell lines up to a concentration of 25 μM and none of the compounds was found toxic to any of the cells. |
| Keywords: | Plasmodium falciparum Artemisinin Tetraoxane Amine conjugates |
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