402477-27-4Relevant academic research and scientific papers
ALLOSTERIC PROTEIN KINASE MODULATORS
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Page/Page column 73-74, (2010/04/30)
The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.
Synthesis and biological evaluation of amide derivatives of (6-chloro-2,3-dihydro-1H-inden-1-yl)acetic acid as potential anti-inflammatory agents with lower gastrointestinal toxicity
Sharma, Meenakshi,Ray, Saumendra Mohan
, p. 626 - 635 (2008/12/21)
A variety of amide derivatives of (6-chloro-2,3-dihydro-1H-inden-1-yl) acetic acid were synthesized and screened for their anti-inflammatory and related biological activities. These compounds were found to be longer acting and showed residual activity exceeding that of standard indomethacin. The studies with SKF-525A, a standard hepatic microsomal enzyme inhibitor showed that probably the test compound per se is the active species. The compound 6y showed best activity profile with ED30 of 6.45 mg/kg however this compound was found to be toxic at 100 mg/kg p.o. Though these compounds exhibited appreciable analgesic and antipyretic activities but they failed to prevent the development of secondary inflammation in adjuvant induced arthritis assay. The compound 6x showed 94% inhibition of acetic acid induced writhing. Studies showed that antagonism of TNF-α is not possibly involved in the mechanism of action of these compounds. However these compounds were found to have only mild ulcerogenic potential at the tested dose level of 100 mg/kg p.o. in comparison to indomethacin.
