27475-19-0Relevant articles and documents
Design, synthesis and SAR analysis of potent BACE1 inhibitors: Possible lead drug candidates for Alzheimer's disease
Tarazi, Hamadeh,Odeh, Raed Abu,Al-Qawasmeh, Raed,Yousef, Imad Abu,Voelter, Wolfgang,Al-Tel, Taleb H.
, p. 1213 - 1224 (2016/11/25)
We have identified potent isophthalic acid derivatives armed with imidazol and indolyl groups as potent β-secretase inhibitors. The most effective analogs demonstrated low nano-molar potency for the BACE1 (β-secretase cleaving enzyme) as measured by FRET (Fluorescence Resonance Energy Transfer) and cell-based (ELISA) assays. Our design strategy followed a traditional SAR approach and was supported by molecular modeling studies based on previously reported hydroxyethylene transition state inhibitor derived from isophthalic acid I. In the FRET assay, the most potent compound, 10a, displayed an IC50value for BACE1 of 75 nM, and exhibited cellular activity with an EC50 value of 0.81 μM. On the other hand, compound 11b was found to be the most potent compound in the cell-based assay with an EC50value of 0.29 μM.
HYDROXAMIC ACID DERIVATIVES AND HDAC8 INHIBITORS
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Paragraph 0025; 0027, (2016/10/07)
PROBLEM TO BE SOLVED: To provide compounds that are highly active and can highly selectively inhibit HDAC8 functionality, and HDAC8 inhibitors. SOLUTION: Each hydroxamic acid derivative comprise a compound of the general formula (1) in the figure, where φ
PYRAZOLO[1,5-A]QUINAZOLIN-5(4H)-ONES AS INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
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Page/Page column 46, (2010/11/29)
The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts or tautomers thereof which are inhibitors of poly(ADP- ribose)polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes mellitus, neurodegenerative diseases, retroviral infections, retinal damage, skin senescence and UV-induced skin damage, and as chemo- or radiosensitizers for cancer treatment.