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Cholinesterase Inhibitory Activity of Some semi-Rigid Spiro Heterocycles: POM Analyses and Crystalline Structure of Pharmacophore Site.
Five compounds with spiro skeleton have been synthesized and tested in vitro for their inhibitory potential against AChE and BChE using ELISA microtiter plate assays at 25 µg/mL and results revealed that three of the spiro compounds tested exert more than 50% inhibition against one of cholinesterases. Expand
Synthesis of novel 2H,8H-pyrano[2,3-f]chromene-2,8-diones from 8-formyl-7-hydroxy-4-methylcoumarin
We report the synthesis of novel 2H,8H-pyrano[2,3-f]chromene-2,8-dione based scaffolds by the reaction of 8-formyl-7-hydroxy-4-methylcoumarin with various active methylene compounds. A mechanism of aExpand
Cytostatic hydroxycoumarin OT52 induces ER/Golgi stress and STAT3 inhibition triggering non-canonical cell death and synergy with BH3 mimetics in lung cancer.
Non-toxic biscoumarin OT52 strongly inhibited proliferation of non-small cell lung cancer cells with KRAS mutations, inhibited stem-like characteristics by reducing aldehyde dehydrogenase expression and abrogated spheroid formation capacity. Expand
Hydroxycoumarin OT-55 kills CML cells alone or in synergy with imatinib or Synribo: Involvement of ER stress and DAMP release.
OT-55 triggered ER stress leading to canonical, caspase-dependent apoptosis and release of danger associated molecular patterns, and promoted phagocytosis of OT-55-treated CML cells by both murine and human monocyte-derived macrophages. Expand
Novel benzofuran–chromone and –coumarin derivatives: synthesis and biological activity in K562 human leukemia cells
Not widely distributed in nature, aurones, (Z)-2-benzylidene-benzofuran-3(2H)-ones, are one of the less common and lesser-known representatives of a flavonoid subclass. Nevertheless, they exhibit aExpand
Advances in Spirocyclic Hybrids: Chemistry and Medicinal Actions.
A structural diversity of spirocyclic hybrids has proved neuroprotective effects, anti-HIV, antiviral and antibacterial activities, which render them impressive synthetic hits for innovative drug conception. Expand
Bis(4-hydroxy-2H-chromen-2-one): synthesis and effects on leukemic cell lines proliferation and NF-κB regulation.
This compound inhibited TNFα-induced NF-κB activation in K-562 and JURKAT cell lines, after 8h of incubation, and exerted mainly cytostatic effects at low doses on both cell lines tested, whereas it decreased JURkAT cell viability starting at 50 μM from 24h of treatment. Expand
Chapter 3 - The Antiinflammatory Potential of Flavonoids: Mechanistic Aspects
Flavonoids are a subclass of phenolic compounds that occur ubiquitously in food plants and vegetables. This class of compounds shares a common 15-carbon structure represented by a benzene ring (A)Expand
One‐Pot Synthesis of Benzopyran‐4‐ones with Cancer Preventive and Therapeutic Potential
A one-pot synthesis of novel benzopyran-4-ones is described. In a tandem reaction, organobase-catalysed Michael addition of (RCOCH2COR2)-C-1 on chromone-3-carboxylic acid led to decarboxylation andExpand
Bis(4-hydroxy-2H-chromen-2-one) Coumarin Induces Apoptosis in MCF-7 Human Breast Cancer Cells Through Aromatase Inhibition
4HC selectively inhibits proliferation of MCF-7cells in vitro, and has inhibitory effects on aromatase gene expression and promoting effects on apoptosis, in MCf-7 cells. Expand