Semisynthesis of novel magnolol-based Mannich base derivatives that suppress cancer cells via inducing autophagy

Development of Membrane-Active Honokiol/Magnolol Amphiphiles as Potent Antibacterial Agents against Methicillin-Resistant Staphylococcus aureus (MRSA)

“… Honokiol and magnolol (Figure ), a class of natural biphenolic compounds, are derived from the root bark of the Chinese medicinal plant Magnolia officinalis (“Hou Po” in Chinese). Honokiol and magnolol have many pharmacological effects, including anticancer, antioxidant, neuroprotective, and antimicrobial activities. − Recently, honokiol and its analogues ( 3 and 4 , Figure ) were reported to exhibit antibacterial activity against S. aureus or Streptococcus mutans probably via a membrane-associated mechanism, but these analogues are not yet considered ideal lead compounds with potential applications. ,, Based on the abovementioned, and to obtain more potent antibacterial honokiol/magnolol analogues, we designed some analogues that bind cationic AMP fragments to honokiol/magnolol.…”

Synthesis and Biological Evaluation of Honokiol Derivatives Bearing 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)oxazol-2(3H)-ones as Potential Viral Entry Inhibitors against SARS-CoV-2

“…Secondly, the nitro group was successfully introduced at the ortho position of hydroxyl groups of the honokiol via nitration reaction to obtain 3,5′-dinitrohonokiol ( 2 ), which was then reduced by SnCl 2 to produce 3,5′-diaminohonokiol ( 3 ). Subsequently, 3,5′-diaminohonokiol ( 3 ) was reacted with urea at 140 °C to obtain another key cyclized product 4 [ 24 ]. Finally, a series of novel honokiol derivatives 6a - p containing various 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)oxazol-2(3 H )-ones were smoothly prepared by reacting compound 4 with the corresponding 2-chloromethyl-5-substituted phenyl-1,3,4-oxadiazoles 5a - p in the presence of K 2 CO 3 and KI [ 25 ].…”

I2-Catalyzed Carbonylation of α-Methylene Ketones to Synthesize 1,2-Diaryl Diketones and Antiviral Quinoxalines in One Pot

“…Compound 4ag displayed IC 50 values of 20.52, 45.01, and 44.45 μM against T47D, MDA-MB-231, and A549 cancer cells, respectively. Of note, the cytotoxic effect of 4ia on MCF-7 and T47D cells was 1.96- and 4.27-fold more potent than that of the positive control of berberine, respectively. Quinoxaline 4ab also displayed 3.94 times stronger cytotoxicity than berberine against T47D cancer cells.…”