863605-34-9Relevant articles and documents
Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity
Bj?rkling, Fredrik,Guguloth, Hanmanthu,Gundepaka, Prasad,Kankala, Shravankumar,Kesari, Chekrapani,Nerella, Srinivas,Rama, Koteshwar Rao,Thota, Niranjan
, p. 1 - 10 (2020/07/21)
A series of fluorophenylpyrazole-picolinamide derivatives were synthesized in high yields using a cross-coupling reaction catalyzed by in situ formed palladium-N-heterocyclic carbenes (Pd-NHCs). The synthesized novel derivatives were evaluated for in vitro anticancer activity against a panel of four human tumor cell lines, HeLa (cervical), A-549 (lung), MCF-7 (breast), and IMR-32 (neuroblastoma). Four compounds, 11c, 11e, 11j, and 11k, showed growth inhibition (low μM) comparable with the standard drug cisplatin, providing a preliminary structure–activity relationship for the series. The present procedure is operationally simple and works with a wide range of substrates and may thus be useful in further compound optimization.
TGF Beta RECEPTOR ANTAGONISTS
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Page/Page column 68; 97; 98, (2018/02/24)
The invention relates generally to compounds that modulate the activity of TGFβR-1 and TGFβR-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
PYRAZOLE SUBSTITUTED IMIDAZOPYRAZINES AS CASEIN KINASE 1 D/E INHIBITORS
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Page/Page column 55-56, (2014/07/08)
The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
KINASE INHIBITORS
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Page/Page column 41, (2010/02/13)
ABSTRACT The present invention provides kinase inhibitors of Formula I: .