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Synthesis and Evaluation of Aminothiazole Derivatives as Hedgehog Pathway Inhibitors
Chemistry & Biodiversity, 2019AbstractA series of aminothiazole derivatives bearing the benzimidazole moiety were synthesized and evaluated in Gli luciferase reporter assays. Lead optimization led to the discovery of potent hedgehog pathway antagonist 18 (2‐[3‐(1H‐benzimidazol‐2‐yl)‐4‐chloroanilino]‐N‐[4‐(trifluoromethyl)phenyl]‐1,3‐thiazole‐4‐carboxamide), with IC50 values in ...
Chiyu Sun +7 more
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Emerging from their burrow: Hedgehog pathway inhibitors for cancer
Expert Opinion on Investigational Drugs, 2016Cancer treatment is moving away from conventional cytotoxic drugs and towards agents that target specific proteins and mechanisms important to cancer development or survival. The Hedgehog Pathway (HhP) is a signal transduction pathway and its constitutive activation is tumorigenic in basal cell carcinoma (BCC).
Gregory N, Gan, Antonio, Jimeno
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Small-Molecule Inhibitors of the Hedgehog Pathway
2011The causal link between uncontrolled Hedgehog (Hh) pathway activation and oncogenesis has inspired the development of small-molecule inhibitors of this developmental signaling pathway. In this chapter, we discuss how a cyclopia-inducing natural product isolated in the 1950s has engendered a pharmacopoeia of compounds that block Hh target gene ...
Ari J. Firestone, James K. Chen
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Recent patents for Hedgehog pathway inhibitors for the treatment of malignancy
Expert Opinion on Therapeutic Patents, 2009There is increasing evidence suggesting that blocking aberrant Hedgehog (Hh) signaling can be a novel therapeutic avenue for the treatment of cancer. During the past decade, efforts from academic and industrial groups have led to the discovery of a variety of Hh pathway inhibitors.This review covers the patent literature related to Hh pathway ...
Martin R, Tremblay +3 more
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Drug Resistance Updates, 2012
Hedgehog (Hh) signaling is a principal component of the morphogenetic code best known to direct pattern formation during embryogenesis. The Hh pathway remains active in adulthood however where it guides tissue regeneration and remodeling and Hh production in the niche plays an important role in maintaining stem cell compartment size.
Souza Queiroz, Karla +2 more
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Hedgehog (Hh) signaling is a principal component of the morphogenetic code best known to direct pattern formation during embryogenesis. The Hh pathway remains active in adulthood however where it guides tissue regeneration and remodeling and Hh production in the niche plays an important role in maintaining stem cell compartment size.
Souza Queiroz, Karla +2 more
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Hedgehog pathway inhibitors in eyelid tumors
Acta OphthalmologicaAims/Purpose: Basal cell carcinoma (BCC) is the most common type of tumor worldwide. Although it has a low capacity for systemic spread, it exhibits a high rate of local invasion. The most frequently affected areas are the face and neck. So far, the most widely used treatment has been surgery in its various forms: excision‐electrodesiccation‐curettage,
Elisa Funes +9 more
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Oral Hedgehog-Pathway Inhibitors for Basal-Cell Carcinoma
New England Journal of Medicine, 2012Basal-cell carcinoma of the skin is the most common cancer worldwide, and its prevalence is increasing, accounting for 80% of nonmelanoma skin cancers.1 In 2006, more than 2.1 million new cases of nonmelanoma skin cancer were treated in the United States.2 Basal-cell carcinoma has many clinical subtypes and can progress to an advanced state in which ...
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Hedgehog pathway inhibitors: a patent review (2009 – present)
Expert Opinion on Therapeutic Patents, 2013The hedgehog (Hh) pathway is a developmental signaling pathway that plays a key role in directing cellular growth and tissue patterning during embryonic development. Dysregulation of Hh signaling has been linked to the development of a variety of human tumors, and numerous drug development programs in both academia and industry are actively exploring ...
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Small molecule inhibitors of the hedgehog signaling pathway for the treatment of cancer
Archives of Pharmacal Research, 2012Over the past decade, the Hedgehog signaling pathway has attracted considerable interest because the pathway plays important roles in the tumorigenesis of several types of cancer as well as developmental processes. It has also been observed that Hedgehog signaling regulates the proliferation and self-renewal of cancer stem cells.
Jeong In, Yun +4 more
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Evaluation of vitamin D3 A-ring analogues as Hedgehog pathway inhibitors
Bioorganic & Medicinal Chemistry Letters, 2012A structure-activity relationship study focusing on the A-ring of vitamin D3 (VD3) was undertaken to elucidate its role in inhibiting the Hedgehog pathway and in mediating anti-cancer effects. Analogues resulting from simple functional group substitution at 3' position of VD3 were evaluated in a variety of biological assays to determine their ability ...
Upasana, Banerjee +2 more
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