1. Synthesis of febrifuginol analogues and evaluation of their biological activities
- Author
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Van Cuong Pham, Giang Vo Thanh, Van Loi Vu, Bich Ngan Truong, Van Hieu Tran, Van Minh Chau, Thi Dao Phi, Huong Doan Thi Mai, and Van Nam Vu
- Subjects
biology ,Chemistry ,Stereochemistry ,Organic Chemistry ,Plasmodium falciparum ,Biological activity ,Glutamic acid ,biology.organism_classification ,Biochemistry ,chemistry.chemical_compound ,Cell culture ,Drug Discovery ,Febrifugine ,Cytotoxic T cell - Abstract
A new series of febrifuginol analogues was prepared from l -glutamic acid. An antimalarial activity evaluation against chloroquine-sensitive (T96) and chloroquine-resistant (K1) Plasmodium falciparum indicated that all the tested compounds had very strong inhibitory activity. Compounds 4 and 17b ′ were inactive against KB, MCF7, HepG2 and LU1 cell lines even at a concentration of 100 μM, while they exhibited significant inhibition towards P. falciparum . Comparison of the antimalarial activity and the cytotoxic properties revealed that the 2′ S isomers were more active than the corresponding 2′ R isomers for this series of febrifuginol analogues, indicating that the C-2′ position is critical for the biological activity of this class of compounds.
- Published
- 2014