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Quinol-based cyclic antioxidant mechanism in estrogen neuroprotection
It is shown that the quinol obtained from a 17β-estradiol derivative was, indeed, able to attenuate glutamate-induced oxidative stress in cultured hippocampus-derived HT-22 cells and may establish the foundation for a rational design of neuroprotective antioxidants focusing on steroidal quinols as unique molecular leads. Expand
Mechanistic investigations on the antioxidant action of a neuroprotective estrogen derivative
This study focused on the mechanistic aspects of hydroxyl radical scavenging by 17beta-butoxy-1,3,5(10)-estratrien-3-ol, a synthetic derivative of 17 beta-estradiol with increased potency to inhibit lipid peroxidation and reduced affinity to estrogen-receptors compared to the endogenous hormone. Expand
Naturally occurring chalcones and their biological activities
The aim of this review is to summarize the various naturally occurring chalcone compounds which have been isolated from different plants to initiate further pharmacobotanical, biotechnological and medicinal studies on the field of chal cone research. Expand
Design, synthesis and antiproliferative activity of some 3-benzylidene-2,3-dihydro-1-benzopyran-4-ones which display selective toxicity for malignant cells.
A series of 3-benzylidene-4-chromanones 1a-l were prepared and their cytotoxicity towards human Molt 4/C8 and CEM T-lymphocytes as well as murine L1210 lymphoid leukemia cells were compared to theExpand
(E)-2-Benzylidenebenzocyclanones, part VIII: spectrophotometric determination of pKa values of some natural and synthetic chalcones and their cyclic analogues
UV–Vis spectrophotometry was used to determine acid dissociation constant (pKa) values of the natural flavonoids phloretin, phlorizin, naringenin, and naringin, as well as 4′-hydroxychalcone,Expand
Conformational and quantitative structure-activity relationship study of cytotoxic 2-arylidenebenzocycloalkanones.
It is revealed that 2-arylidene-1-benzosuberones are a group of useful cytotoxic agents, and in particular 3k serves as a prototypic molecule for subsequent structural modifications. Expand
In vitro antiproliferative and antiangiogenic effects of synthetic chalcone analogues.
In non-toxic concentrations, chalcone 3 inhibited VEGF-induced migration of human umbilical vein endothelial cells and decreased secretion of matrix metalloproteinase and vascular endothelial growth factor. Expand
Mechanistic insights into the direct antioxidant effects of estrogens
Free‐radical scavenging by estrogens has been implicated as one of their non‐genomic (estrogen‐receptor independent) mechanisms of cytoprotection. This activity is associated with the presence of theExpand
Centrally acting and metabolically stable thyrotropin-releasing hormone analogues by replacement of histidine with substituted pyridinium.
The benefits of the prodrug approach on the pharmacokinetics and brain uptake/retention of pyridinium-containing TRH analogues (measured by in vivo microdialysis sampling) upon systemic administration are demonstrated. Expand
Integration of mass spectrometry into early-phase discovery and development of central nervous system agents.
Making atmospheric-pressure ionization mass spectrometry an integral part of the process has played a major role in increasing throughput, selectivity, specificity and detection sensitivity and thereby providing useful information about the extent or mechanism of transport and metabolic activation/inactivation in early-phase discovery and development of CNS agents. Expand