Design,synthesis and biological evaluation of benzyl 2-(1H-imidazole-1-yl) pyrimidine analogues as selective and potent Raf inhibitors |
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| Institution: | 1. Department of Pharmacy, College of Pharmacy & Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan, Kyeonggi-do 426-791, Republic of Korea;2. College of Pharmacy & Graduate School of Pharmaceutical Sciences, Global Top 5 Research Program, Ewha Womans University, 11-1 Daehyun-Dong, Seodaemun-Gu, Seoul 120-750, Republic of Korea;1. College of Pharmacy & Graduate School of Pharmaceutical Sciences, Global Top 5 Research Program, Ewha Womans University, 11-1 Daehyun-Dong, Seodaemun-Gu, Seoul 120-750, Republic of Korea;2. Department of Pharmacy, College of Pharmacy, Institute of Pharmaceutical Science and Technology, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan, Kyeonggi-do 426-791, Republic of Korea;1. Chemistry Department, Faculty of Arts and Science, Dumlup?nar University, 43100 Kütahya, Turkey;2. Università degli Studi di Firenze, NEUROFARBA Dept., Sezione di Scienze Farmaceutiche e Nutraceutiche, 50019 Sesto Fiorentino (Florence), Italy;3. Biochemistry Department, Faculty of Arts and Science, Dumlup?nar University, 43100 Kütahya, Turkey;1. Department of Pharmacy, Faculty of Biological Sciences, Quaid-e-Azam University, Islamabad, Pakistan;2. Department of Pharmacy, Abasyn University Peshawar, KPK, Pakistan;3. Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, DOW University of Health Sciences, 74200, Karachi, Pakistan;4. Institute of Pharmaceutical Sciences, Khyber Medical University Peshawar, Pakistan;5. District Headquarter Hospital Khushab, Punjab Pakistan, Pakistan;6. Department of Pharmaceutics, Faculty of Pharmacy, University of Bonn, 53121, Bonn, Germany;7. Department of Pharmacy, University of Central Punjab, Lahore, Pakistan;8. National University of Medical Sciences, Rawalpindi, Pakistan;1. Riphah Institute of Pharmaceutical Sciences, Riphah International University, Islamabad, Pakistan;2. Department of Pharmacy, Quaid-i-Azam University, Islamabad, Pakistan;3. Faculty of Pharmacy, University of Central Punjab, Lahore, Pakistan;4. College of Pharmacy, Institute of Pharmaceutical Science and Technology, Hanyang University, Ansan, Gyeonggi, Republic of Korea;1. Department of Medicine, Massachusetts General Hospital and Harvard Medical School, Boston, MA 02129, USA;2. Department of Medicine, Brigham and Women''s Hospital and Harvard Medical School, Boston, MA 02115, USA;3. The Broad Institute of MIT and Harvard, Cambridge, MA 02142, USA;4. Department of Biomedicine, Molecular Nephrology, University of Basel, Basel 4031, Switzerland |
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| Abstract: | The synthesis of a novel series of (4-aminobenzyl/benzoyl)-1H-imidazol-1-yl pyrimidin-2-yl derivatives 9, 10, 18, 19 and their in vitro antiproliferative activities against the A375P human melanoma cell line and the U937 human leukemic monocyte lymphoma cell line are described. Potent antiproliferative effects were found from 9l, 9s and 10c; 10c was found to be a highly potent and selective BRAF V600E and CRAF inhibitor (IC50 = 38.3 nM and 8.79 nM). |
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| Keywords: | Antiproliferative activity Melanoma BRAF V600E CRAF Selectivity |
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