5,7,8-Trimethoxydictamnine is a quinoline alkaloid that has been found inRutaceaeand has antimalarial activity.1It is active against chloroquine-sensitive and -resistant strains ofP. falciparum(IC50s =19.9 and 5.72 μg/ml, respectively). 1.Basco, L.K.M., S., Skaltsounis, A.-L., Ravvelomanantsoa, N., et al.In vitro activities of furoquinoline and acridone alkaloids against Plasmodium falciparumAntimicrob. Agents Chemother.38(5)1169-1171(1994)
Evoxanthine is an alkaloid that has been found in O. renieri and has antimalarial and anticancer activities.1,2 It is active against P. falciparum with an IC50 value of 67.6 μg ml.1 Evoxanthine decreases proliferation of nine sensitive and drug-resistant cancer cell lines (IC50s = 6.11-80.99 μM).2 |1. Khalid, S.A., Farouk, A., Geary, T.G., et al. Potential antimalarial candidates from African plants: And in vitro approach using Plasmodium falciparum. J. Ethnopharmacol. 15(2), 201-209 (1986).|2. Kuete, V., Fouotsa, H., Mbaveng, A.T., et al. Cytotoxicity of a naturally occurring furoquinoline alkaloid and four acridone alkaloids towards multi-factorial drug-resistant cancer cells. Phytomedicine 22(10), 946-951 (2015).
STING agonist 12b is an agonist of stimulator of interferon genes (STING).1It binds to STING (Kd= 26.4 μM) and induces interferon reporter gene expression in cells expressing human or mouse STING (EC50s = 7.45 and 10.23 μM, respectively). STING agonist 12b (40 μM) induces expression of TNF-a, IL-6, IP-10, and IL-1b in THP-1 cells. 1.Hou, S., Lan, X.-j., Li, W., et al.Design, synthesis and biological evaluation of acridone analogues as novel STING receptor agonistsBioorg. Chem.95103556(2020)
Topoisomerase II inhibitor 3 (Compound 6 h) is an acridone derivative that acts as a Type II DNA topoisomerase (topo II) inhibitor. It specifically inhibits the topo IIα β subtypes, with an IC50 value of 0.17 μM for topo IIα and 0.23 μM for topo IIβ. This compound elicits significant DNA damage and induces apoptosis by triggering the loss of mitochondrial membrane potential [1].