cc-401 and nintedanib

cc-401 has been researched along with nintedanib* in 1 studies

Other Studies

1 other study(ies) available for cc-401 and nintedanib

Article	Year
Discovery of a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth. Bioorganic & medicinal chemistry, 2017, 05-01, Volume: 25, Issue:9 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. Topics: Acetanilides; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Humans; Indoles; Molecular Docking Simulation; Myeloid Cell Leukemia Sequence 1 Protein; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases	2017

Article

Year

Discovery of a potent inhibitor of MELK that inhibits expression of the anti-apoptotic protein Mcl-1 and TNBC cell growth.

Bioorganic & medicinal chemistry, 2017, 05-01, Volume: 25, Issue:9

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.

Topics: Acetanilides; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Humans; Indoles; Molecular Docking Simulation; Myeloid Cell Leukemia Sequence 1 Protein; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases

2017