Novel artemisinin-1,2,3-triazole derivatives show significant antiproliferative activity, and induce apoptosis and ROS generation and arrest the cell cycle at the G2/M phase.
Twenty one chalcone derivatives were synthesized using Claisen-Schmidt condensation, their antimalarial activity against Plasmodium falciparum was determined and quantitative structureactivity relationship (QSAR) was developed. Condensation of substituted acetophenones with various aromatic aldehydes at room temperature gave chalcones in 75-96% yield. Chalcones are secondary metabolites of terrestrial plants, precursors for the biosynthesis of flavonoids and exhibit various biological activities. Antiplasmodial IC 50 (half-maximal inhibitory concentration) activity of a compound against malaria parasites in vitro provides a good first screen for identifying the antimalarial potential of the compound. The most active compound was Trans-3-(1H-indol-3-yl)-1-(2'-hydroxyphenyl)-2-propen-1-one (1b) with IC 50 of 2.1 µM/L. Molecular mechanism was explored through in silico docking & ADMET studies.
Isoliquiritigenin (ISL, 1) and liquiritigenin (LTG, 2) were isolated from the rhizomes of Glycyrrhiza glabra. In an attempt to develop potent and selective antituberculosis agents, a series of ISL analogues were synthesized mainly via acid-and base-catalyzed ClaisenSchmidt condensation reaction for their antitubercular activity. Compared to ISL (MIC = 25 lg/mL), analogues 5, 8, and 10 showed similar antitubercular activity, but, interestingly, 6, 7, and 15 exhibited twofold higher activity (MIC = 12.5 lg/mL) over ISL, against Mycobacterium tuberculosis. Among the LTG derivatives, LTG 4 0 -acetate and LTG-oxime were found to be as active (MIC = 25 lg/ mL) as LTG. It is the first report on antimycobacterial activity of these ISL-and LTG-based derivatives. Molecular docking and in silico ADME studies revealed that compounds 6, 7, and 15 are potent inhibitors of M. tuberculosis H 37 Rv alanine dehydrogenase and showed compliance with standard parameters of drug likeness.
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