Results 211 to 220 of about 1,857,972 (264)

GDC-0449—A Potent Inhibitor of the Hedgehog Pathway

Bioorganic and Medicinal Chemistry Letters, 2009
SAR for a wide variety of heterocyclic replacements for a benzimidazole led to the discovery of functionalized 2-pyridyl amides as novel inhibitors of the hedgehog pathway. The 2-pyridyl amides were optimized for potency, PK, and drug-like properties by modifications to the amide portion of the molecule resulting in 31 (GDC-0449).
Lee L. Rubin   +2 more
exaly   +3 more sources

Potent Inhibitors of the Hedgehog Signaling Pathway

Journal of Medicinal Chemistry, 2008
A small family of phenyl quinazolinone ureas is reported as potent modulators of Hedgehog protein function. Preliminary SAR studies of the urea substituent led to a nanomolar Hedgehog antagonist.
Shirley A, Brunton   +6 more
openaire   +2 more sources

Treatment of Medulloblastoma With Hedgehog Pathway Inhibitor GDC-0449 [PDF]

open access: yesNew England Journal of Medicine, 2009
Medulloblastoma is the most common malignant brain tumor in children. Aberrant activation of the hedgehog signaling pathway is strongly implicated in the development of some cases of medulloblastoma. A 26-year-old man with metastatic medulloblastoma that was refractory to multiple therapies was treated with a novel hedgehog pathway inhibitor, GDC-0449;
Charles Rudin   +2 more
exaly   +3 more sources

Discovery of the Hedgehog Pathway Inhibitor Pipinib That Targets PI4KIIIß [PDF]

open access: yesAngewandte Chemie - International Edition, 2019
AbstractThe Hedgehog (Hh) signaling pathway is crucial for vertebrate embryonic development, tissue homeostasis and regeneration. Hh signaling is upregulated in basal cell carcinoma and medulloblastoma and Hh pathway inhibitors targeting the Smoothened (SMO) protein are in clinical use.
Radim Nencka   +2 more
exaly   +6 more sources

Hedgehog pathway and smoothened inhibitors in cancer therapies

Anti-Cancer Drugs, 2018
The hedgehog (Hh) pathway plays an important role in cancer development and maintenance, as ~25% of all cancers have aberrant Hh pathway activation. Targeted therapy for inhibition of the Hh pathway was thought to be promising for achieving clinical response in the Hh-dependent cancers.
Kirti K, Chahal   +2 more
openaire   +2 more sources

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