Design, synthesis and optimization of 7-substituted-pyrazolo[4,3-b]pyridine ALK5 (activin receptor-like kinase 5) inhibitors.
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J. Lawson | M. Hixon | D. Dougan | M. Sabat | N. Scorah | R. Kamran | Joy Atienza | Haixia Wang | Mark Sabat | Ruhi Kamran | J. David Lawson
[1] J. Lawson,et al. Design, synthesis and optimization of novel Alk5 (activin-like kinase 5) inhibitors. , 2016, Bioorganic & medicinal chemistry letters.
[2] S. Estrem,et al. Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway , 2015, Drug design, development and therapy.
[3] M. Abdullah,et al. Inhibition of transforming growth factor-β via the activin receptor-like kinase-5 inhibitor attenuates pulmonary fibrosis. , 2015, Molecular medicine reports.
[4] Jeong-Seok Nam,et al. EW-7197 inhibits hepatic, renal, and pulmonary fibrosis by blocking TGF-β/Smad and ROS signaling , 2014, Cellular and Molecular Life Sciences.
[5] K. S. Rao,et al. Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. , 2014, Journal of medicinal chemistry.
[6] I. Fabregat,et al. TGF-beta signaling in cancer treatment. , 2014, Current pharmaceutical design.
[7] E. Terpos,et al. Activin receptor antagonists for cancer-related anemia and bone disease , 2013, Expert opinion on investigational drugs.
[8] R. Akhurst,et al. Complexities of TGF-β Targeted Cancer Therapy , 2012, International journal of biological sciences.
[9] Mostofa A Hena,et al. Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring. , 2012, Bioorganic & medicinal chemistry letters.
[10] L. Ling,et al. Tgf-beta type I receptor (Alk5) kinase inhibitors in oncology. , 2011, Current pharmaceutical biotechnology.
[11] J. Render,et al. An Activin Receptor-Like Kinase 5 Inhibitor Reduces Collagen Deposition in a Rat Dermal Incision Wound Healing Model , 2011, Plastic and reconstructive surgery.
[12] M. Anderton,et al. Induction of Heart Valve Lesions by Small-Molecule ALK5 Inhibitors , 2011, Toxicologic pathology.
[13] David J. Nesbitt,et al. Definition of the hydrogen bond (IUPAC Recommendations 2011) , 2011 .
[14] R. Obach. Predicting clearance in humans from in vitro data. , 2011, Current topics in medicinal chemistry.
[15] F. Gellibert,et al. Design of novel quinazoline derivatives and related analogues as potent and selective ALK5 inhibitors. , 2009, Bioorganic & medicinal chemistry letters.
[16] R. Campbell,et al. Optimization of a dihydropyrrolopyrazole series of transforming growth factor-beta type I receptor kinase domain inhibitors: discovery of an orally bioavailable transforming growth factor-beta receptor type I inhibitor as antitumor agent. , 2008, Journal of medicinal chemistry.
[17] P. Leeson,et al. The influence of drug-like concepts on decision-making in medicinal chemistry , 2007, Nature Reviews Drug Discovery.
[18] Randy J. Read,et al. Phaser crystallographic software , 2007, Journal of applied crystallography.
[19] A. Hopkins,et al. Ligand efficiency: a useful metric for lead selection. , 2004, Drug discovery today.
[20] C. Chuaqui,et al. Successful shape-Based virtual screening: The discovery of a potent inhibitor of the type I TGFβ receptor kinase (TβRI) , 2003 .
[21] A. Reith,et al. SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7. , 2002, Molecular pharmacology.
[22] D E McRee,et al. XtalView/Xfit--A versatile program for manipulating atomic coordinates and electron density. , 1999, Journal of structural biology.
[23] A. Vagin,et al. MOLREP: an Automated Program for Molecular Replacement , 1997 .
[24] G. Murshudov,et al. Refinement of macromolecular structures by the maximum-likelihood method. , 1997, Acta crystallographica. Section D, Biological crystallography.
[25] Tim Morris,et al. Physiological Parameters in Laboratory Animals and Humans , 1993, Pharmaceutical Research.
[26] Z. Otwinowski,et al. [20] Processing of X-ray diffraction data collected in oscillation mode. , 1997, Methods in enzymology.