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…
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.
Synthesis and biological evaluation of resveratrol and analogues as apoptosis-inducing agents.
- M. Roberti, Daniela Pizzirani, M. Tolomeo
- Chemistry, BiologyJournal of Medicinal Chemistry
- 1 July 2003
Data indicate unambiguously that structural alteration of the stilbene motif of resveratrol can be extremely effective in producing potent apoptosis-inducing agents.
Pterostilbene and 3'-hydroxypterostilbene are effective apoptosis-inducing agents in MDR and BCR-ABL-expressing leukemia cells.
Small molecule aurora kinases inhibitors.
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.
Berberine and its metabolites: relationship between physicochemical properties and plasma levels after administration to human subjects.
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.
Non-ATP competitive protein kinase inhibitors.
In this review small molecules capable of inducing the DFG-out conformation are reported, especially focusing on structural feature, SAR and biological properties.
Galloflavin (CAS 568‐80‐9): A Novel Inhibitor of Lactate Dehydrogenase
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.
Heterocyclic and phenyl double-bond-locked combretastatin analogues possessing potent apoptosis-inducing activity in HL60 and in MDR cell lines.
The data suggest unambiguously that structural alteration of the stilbene motif of CA-4 can be extremely effective in producing potent apoptosis-inducing agents.
Stilbene-based anticancer agents: resveratrol analogues active toward HL60 leukemic cells with a non-specific phase mechanism.
Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-β aggregation and to exert anticholinesterase and antioxidant effects.
- E. Nepovimova, Elisa Uliassi, M. Bolognesi
- Biology, ChemistryJournal of Medicinal Chemistry
- 10 October 2014
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.