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Probing the Binding Sites and Mechanisms of Action of Two Human Ether-a-go-go-Related Gene Channel Activators, 1,3-bis-(2-Hydroxy-5-trifluoromethyl-phenyl)-urea (NS1643) and
TLDR
It is suggested that PD may work as a “pore-modifier” of the hERG channel: it binds to the outer vestibule/pore entrance of hERG and increases current amplitudes by promoting channel activation while retarding inactivation. Expand
Synthesis and biological evaluation of resveratrol and analogues as apoptosis-inducing agents.
TLDR
Data indicate unambiguously that structural alteration of the stilbene motif of resveratrol can be extremely effective in producing potent apoptosis-inducing agents. Expand
Pterostilbene and 3'-hydroxypterostilbene are effective apoptosis-inducing agents in MDR and BCR-ABL-expressing leukemia cells.
TLDR
The data show that pterostilbene and particularly 3,5-hydroxypterostILbene are interesting antitumor natural compounds that may be useful in the treatment of resistant hematological malignancies, including imatinib, non-responsive neoplasms. Expand
Berberine and its metabolites: relationship between physicochemical properties and plasma levels after administration to human subjects.
TLDR
Results indicate that the higher plasma concentration of 2 was a consequence of a more efficient intestinal absorption, suggesting that berberrubine is potentially more pharmacologically active than berberine. Expand
Non-ATP competitive protein kinase inhibitors.
TLDR
In this review small molecules capable of inducing the DFG-out conformation are reported, especially focusing on structural feature, SAR and biological properties. Expand
Stilbene-based anticancer agents: resveratrol analogues active toward HL60 leukemic cells with a non-specific phase mechanism.
TLDR
A peculiar behavior of 6b was found that caused a decrease of cells in all phases of cell cycle and a proportional increase of apoptotic cells and the potent pro-apoptotic activity shown by compound 6b and its effects on cell cycle make this compound of great interest for further investigations. Expand
Small molecule aurora kinases inhibitors.
TLDR
The specific targeting of these kinases could result in highly active drugs with minimal collateral host toxicity, and the combination of Aurora inhibitors with other chemotherapeutic agents may open new opportunities in cancer chemotherapy. Expand
Galloflavin (CAS 568‐80‐9): A Novel Inhibitor of Lactate Dehydrogenase
TLDR
Galloflavin inhibits both human LDH isoforms by preferentially binding the free enzyme, without competing with the substrate or cofactor, and is the only biochemical effect described for gall oflavin. Expand
Heterocyclic and phenyl double-bond-locked combretastatin analogues possessing potent apoptosis-inducing activity in HL60 and in MDR cell lines.
TLDR
The data suggest unambiguously that structural alteration of the stilbene motif of CA-4 can be extremely effective in producing potent apoptosis-inducing agents. Expand
Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects.
TLDR
When ex vivo results were combined with in vitro studies, these two compounds emerged to be promising multitarget lead candidates worthy of further pursuit, and crossed the blood-brain barrier, as demonstrated in ex vivo experiments with rats. Expand
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