Discovery,synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors |
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| Institution: | 1. Warren Center for Neuroscience Drug Discovery, Vanderbilt University, Nashville, TN 37232, USA;2. Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE 68198-6125, USA;3. Department of Pharmacology, Vanderbilt University, Nashville, TN 37232, USA;4. Department of Chemistry, Vanderbilt University, Nashville, TN 37232, USA;5. Department of Biochemistry, Vanderbilt University, Nashville, TN 37232, USA;6. Division of Cardiovascular Medicine, University of Maryland School of Medicine, Baltimore, MD 21201, USA;1. Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India;2. Department of Regulatory Toxicology, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad 500037, India;3. Medicinal Chemistry and Biotechnology Division, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad 500007, India;4. School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India;1. Laboratoire de Biotechnologies Végétales et Ethnobotanique, Faculté des Sciences de la Nature et de la Vie, Université de Bejaia, Bejaia, Algeria;2. CIBER-EHD, Department of Pharmacology, Centre for Biomedical Research (CIBM), University of Granada, Granada, Spain;3. Instituto de Investigación Biosanitaria de Granada (ibs.GRANADA), Granada, Spain;4. Servicio de Digestivo, Hospital Universitario Virgen de las Nieves, 18012 Granada, Spain;1. Department of Pharmaceutical Chemistry, Gokaraju Rangaraju College of Pharmacy, Bachupally, Kukatpally, Hyderabad 500090, India;2. Department of Pharmacology, National Institute of Pharmaceutical Education and Research, Balanagar, Hyderabad 500042, India;3. Department of Chemistry, University College of Science and Faculty of Pharmacy, Osmania University, Hyderabad 500007, India;1. Department of Oral Pathology and Regenerative Medicine, School of Dentistry, IHBR, Kyungpook National University, Daegu 41940, Republic of Korea;2. Department of Food Science and Biotechnology, Daegu University, Gyeongsan 38453, Republic of Korea;3. Cell and Matrix Research Institute (CMRI), Kyungpook National University, Daegu 41940, Republic of Korea;4. Department of Marine Life Sciences, School of Marine Biomedical Sciences, Jeju National University, Jeju 63243, Republic of Korea;5. Department of Biochemistry, College of Korean Medicine, Dong-Eui University, Busan 47227, Republic of Korea;6. College of Pharmacy, CMRI, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Republic of Korea;7. Department of Biology, College of Natural Sciences, Kyungpook National University, Daegu 41566, Republic of Korea;8. Department of Molecular Medicine, CMRI, School of Medicine, Kyungpook National University, Daegu 41944, Republic of Korea;1. Drug Discovery Research, Astellas Pharma Inc.; 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan |
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| Abstract: | The activin-like kinases are a family of kinases that play important roles in a variety of disease states. Of this class of kinases, ALK2, has been shown by a gain-of-function to be the primary driver of the childhood skeletal disease fibrodysplasia ossificans progressiva (FOP) and more recently the pediatric cancer diffuse intrinsic pontine glioma (DIPG). Herein, we report our efforts to identify a novel imidazo1,2-a]pyridine scaffold as potent inhibitors of ALK2 with good in vivo pharmacokinetic properties suitable for future animal studies. |
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| Keywords: | BMP inhibitors Activin-like kinase inhibitors ALK2 ALK3 |
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