Unsymmetrical Bisquinolines with High Potency against P. falciparum Malaria
Abstract
:1. Introduction
2. Results
Compound | Activity (IC50; nM) | Cytotoxicity | Structure | ||
---|---|---|---|---|---|
D6 | Dd2 | 7G8 | (LC50; nM) Mouse Spleen Lymphocytes | ||
CQ | 6.9 | 102 | 106 | 12,400 | |
PPQ | 0.7 | 1.5 | | ||
1 | 1.3 | 4.1 | 7.4 | | |
2 [46] | 2.4 | 3.7 | 1.5 | 1100 | |
3 | 1.5 | 5.0 | 1600 | | |
4 (DM1157) [46,47] | 0.2 | 2.2 | 1.8 | 6500 | |
5 [45] | 0.4 | 0.7 | 0.1 | | |
6 | 0.15 | 0.36 | 0.33 | 190 | |
7 | 4.9 | 9.8 | 25 | | |
8 | 0.68 | 2.1 | 0.63 | | |
9 | 0.68 | 2.1 | 0.41 | | |
10 | 15 | 89 | 106 | | |
11 | 3.0 | <2.5 | <2.5 | | |
12 | 4.5 | <2.5 | <2.5 | | |
13 | 33 | 56 | 100 | |
3. Discussion
4. Materials and Methods
4.1. General Synthetic Methods
4.2. Characterization of Products
Example Synthesis: Compound 6
4.3. In Vitro Studies on Inhibition of P. falciparum Parasite Growth
5. Conclusions
Supplementary Materials
Author Contributions
Funding
Acknowledgments
Conflicts of Interest
References
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Liebman, K.M.; Burgess, S.J.; Gunsaru, B.; Kelly, J.X.; Li, Y.; Morrill, W.; Liebman, M.C.; Peyton, D.H. Unsymmetrical Bisquinolines with High Potency against P. falciparum Malaria. Molecules 2020, 25, 2251. https://doi.org/10.3390/molecules25092251
Liebman KM, Burgess SJ, Gunsaru B, Kelly JX, Li Y, Morrill W, Liebman MC, Peyton DH. Unsymmetrical Bisquinolines with High Potency against P. falciparum Malaria. Molecules. 2020; 25(9):2251. https://doi.org/10.3390/molecules25092251
Chicago/Turabian StyleLiebman, Katherine M., Steven J. Burgess, Bornface Gunsaru, Jane X. Kelly, Yuexin Li, Westin Morrill, Michael C. Liebman, and David H. Peyton. 2020. "Unsymmetrical Bisquinolines with High Potency against P. falciparum Malaria" Molecules 25, no. 9: 2251. https://doi.org/10.3390/molecules25092251