Synthesis of febrifuginol analogues and evaluation of their biological activities |
| |
| Institution: | 1. Department of Orthopaedic Surgery, University of Tsukuba, Ibaraki, Japan;2. National Institute of Advanced Industrial Science and Technology, Tsukuba, Ibaraki, Japan;1. Satiate Research & Anatech Pvt. Ltd., HSIIDC, Barwala, Haryana, India;2. I. K. Gujral Punjab Technical University, Jalandhar, Punjab, India;3. Laboratory for Organic & Microwave-Assisted Chemistry (LOMAC), Department of Chemistry, University of Leuven (KU Leuven), Leuven, Belgium;1. University of Auckland, New Zealand;2. Unitec Institute of Technology, New Zealand |
| |
| 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. |
| |
| Keywords: | Febrifuginol Febrifugine Synthesis Cytotoxic Antimalarial |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
