864688-87-9Relevant articles and documents
Discovery of a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth
Edupuganti, Ramakrishna,Taliaferro, Juliana M.,Wang, Qiantao,Xie, Xuemei,Cho, Eun Jeong,Vidhu, Fnu,Ren, Pengyu,Anslyn, Eric V.,Bartholomeusz, Chandra,Dalby, Kevin N.
, p. 2609 - 2616 (2017)
Despite recent advances in molecularly directed therapy, triple negative breast cancer (TNBC) remains one of the most aggressive forms of breast cancer, still without a suitable target for specific inhibitors. Maternal embryonic leucine zipper kinase (MELK) is highly expressed in TNBC, where level of overexpression correlates with poor prognosis and an aggressive disease course. Herein, we describe the discovery through targeted kinase inhibitor library screening, and structure-guided design of a series of ATP-competitive indolinone derivatives with subnanomolar inhibition constants towards MELK. The most potent compound, 17, inhibits the expression of the anti-apoptotic protein Mcl-1 and proliferation of TNBC cells exhibiting selectivity for cells expressing high levels of MELK. These studies suggest that further elaboration of 17 will furnish MELK-selective inhibitors with potential for development in preclinical models of TNBC and other cancers.
INDOLINONE DERIVATIVES AS INHIBITORS OF MATERNAL EMBRYONIC LEUCINE ZIPPER KINASE
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Page/Page column 65, (2018/09/20)
The present disclosure relates to indolinone compounds, compositions, and methods for the inhibition of maternal embryonic leucine zipper kinase (MELK). The present disclosure further relates to indolinone compounds, compositions, and methods for the treatment or prevention of a cancer (for example, triple negative breast cancer).
Alkyl-containing 5-acylindolinones, the preparation thereof and their use as medicaments
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Page/Page column 10, (2008/06/13)
The present invention relates to alkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have val
Cycloalkyl - containing 5-acylindolinones, the preparation thereof and their use as medicaments
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Page/Page column 10, (2008/06/13)
The present invention relates to cycloalkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined as in claims 1 to 6, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).
NOVEL ALKYL-CONTAINING 5-ACYLINDOLINONES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICAL PRODUCTS
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Page/Page column 25, (2008/06/13)
The invention relates to alkyl-containing 5-acylindolinones of the general formula (I), where R1 to R3 are as defined in claim 1, and to tautomers, enantiomers, diastereomers, mixtures and salts thereof with valuable pharmacological
NOVEL CYCLOALKYL-CONTAINING 5-ACYLINDOLINONES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICAL PRODUCTS
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Page/Page column 25, (2008/06/13)
The invention relates to cycloalkyl-containing 5-acylindolinones of the general formula (I), where R1 to R3 are as defined in claims 1 to 6, and to tautomers, enantiomers, diastereomers, mixtures and salts thereof with valuable pharmacological properties, more particularly an inhibitory effect on protein kinases, more particularly an inhibitory effect on the activity of glycogen synthase kinase (GSK-3).
NOVEL ARYL-CONTAINING 5-ACYLINDOLINONES, THE PRODUCTION THEREOF AND THEIR USE AS MEDICAMENTS
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Page/Page column 25, (2010/02/14)
The invention relates to aryl-containing 5-acylindolinones of general formula (I) in which R1 to R3 are defined as in Claims 1 to 7, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, all of which having valuable
Aryl-containing 5-acylindolinones, the preparation thereof and their use as medicaments
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Page/Page column 8, (2010/02/14)
The present invention relates to aryl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valu
