7126-50-3Relevant articles and documents
Identification of azepinone fused tetracyclic heterocycles as new chemotypes with protein kinase inhibitory activities
Psarra, Vassiliki,Fousteris, Manolis A.,Hennig, Lothar,Bantzi, Marina,Giannis, Athanassios,Nikolaropoulos, Sotiris S.
supporting information, p. 2376 - 2385 (2016/04/26)
The design and synthesis of small tetracyclic heterocycles which bear two new regioisomeric 2-carboxyethyl-1H-pyrrole-annulated indoloazepinone scaffolds is described. An azepinone motif, which is inherent in the structures of many well studied protein kinase inhibitors, serves as prominent structural feature of the new compounds. Concise access to the new regioisomeric tetracyclic derivatives was accomplished through amide coupling of appropriate pyrrole and indole precursors followed by an intramolecular Heck coupling reaction of the intermediate amide conjugates. Preliminary evaluation of newly synthesized tetracyclic molecules against a panel of protein kinases indicated their inhibitory activities and revealed promising selectivity profiles. The new compounds displayed no significant antiproliferative activity against MCF-7 cancer cells. Interestingly, derivative 19a exhibited selective TAK1 kinase inhibitory activity and figures as a promising chemotype for the discovery of new TAK1 inhibitors.
5-sulfonamido-substituted indolinone compounds as protein kinase inhibitors
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Page/Page column 16, (2010/02/08)
The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
SUBSTITUTED PYRAZOLE ANGIOTENSIN II ANTAGONISTS
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, (2008/06/13)
Substituted pyrazoles such as STR1 and their pharmaceutically suitable salts are useful as antihypertensive agents and for treatment of congestive heart failure.