- Discovery of a sulfamate-based steroid sulfatase inhibitor with intrinsic selective estrogen receptor modulator properties
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Steroid sulfatase (STS), the enzyme which converts inactive sulfated steroid precursors into active hormones, is a promising therapeutic target for the treatment of estrogen-sensitive breast cancer. We report herein the synthesis and in vitro study of dua
- Ouellet, Charles,Maltais, René,Ouellet, étienne,Barbeau, Xavier,Lagüe, Patrick,Poirier, Donald
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- Multifunctional cholinesterase inhibitors for Alzheimer's disease: Synthesis, biological evaluations, and docking studies of o/p-propoxyphenylsubstituted-1H-benzimidazole derivatives
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This study indicates the synthesis, cholinesterase (ChE) inhibitory activity, and molecular modeling studies of 48 compounds as o- and p-(3-substitutedethoxyphenyl)-1H-benzimidazole derivatives. According to the ChE inhibitor activity results, generally, para series are more active against acetylcholinesterase (AChE) whereas ortho series are more active against butyrylcholinesterase (BuChE). The most active compounds against AChE and BuChE are compounds A12 and B14 with IC50 values of 0.14 and 0.22 μM, respectively. Additionally, the most active 16 compounds against AChE/BuChE were chosen to investigate the neuroprotective effects, and the results indicated that most of the compounds have free radical scavenging properties and show their effects by reducing free radical production; moreover, some of the compounds significantly increased the viability of SH-SY5Y cells exposed to H2O2. Overall, compounds A12 and B14 with potential AChE and BuChE inhibitory activities, high neuroprotection against H2O2-induced toxicity, free radical scavenging properties, and metal chelating abilities may be considered as lead molecules for the development of multi-target-directed ligands against Alzheimer's disease.
- Sar?kaya, G?rkem,?oban, Güne?,Parlar, Sülünay,Tarikogullari, Ayse H.,Armagan, Güliz,Erdo?an, Mümin A.,Alptüzün, Vildan,Alpan, Ay?e S.
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- COMPOUNDS FOR THE TREATMENT OF HORMONE-DEPENDENT DISEASES
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Provided are compounds of general formula A and A', wherein X1 and X2 are each C, CH or N; R3 and R4 are each H, optionally substituted C1-C30 saturated or unsaturated chemical group, or to
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Paragraph 0046; 0064; 0065; 0066
(2015/03/13)
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- Substituted amides and sulfonamides containing a heterocyclic group having antiinflammatory activity
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Compounds having the formula STR1 wherein R1 is alkyl, cycloalkyl or aryl; R2 is acyl or sulfonyl; R3 is a nitrogen containing heterocyclic group; A1 is a saturated bond or an alkylene group having 1 to 4 carbon
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