Triazolopyridazine derivatives: Synthesis,cytotoxic evaluation,c-Met kinase activity and molecular docking |
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| Affiliation: | 1. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt;2. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, October 6 University, Giza, Egypt;3. Pharmaceutical Chemistry Department, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Giza, Egypt;4. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr Elini St., Cairo 11562, Egypt;1. Department of Biochemistry, Faculty of Science, University of Tabuk, Saudi Arabia;2. Department of Chemistry, Biochemistry Speciality, Faculty of Science, Cairo University, Egypt;3. Department of Chemistry, Organic Chemistry Speciality, Faculty of Science, Cairo University, Egypt;4. Department of Biochemistry, El Sahel Teaching Hospital, Cairo, Egypt;5. Department of Radiotherapy, Children’s Cancer Hospital Egypt (CCHE), Cairo, Egypt;1. Key Laboratory of Structure-Based Drug Design and Discovery (Shenyang Pharmaceutical University), Ministry of Education, 103 Wenhua Road, Shenhe District, Shenyang 110016, PR China;2. College of Pharmacy of Liaoning University, Key Laboratory of New Drug Research and Development of Liaoning Province, 66 Chongshan Road, Huanggu District, Shenyang 110036, PR China;1. Guizhou Provincial Key Laboratory of Pharmaceutics, State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550004, China;2. Guizhou Provincial Engineering Research Center for the Development and Application of Ethnic Medicine and TCM, Guizhou Medical University, Guiyang 550004, China;3. School of Pharmacy, Guizhou Medical University, Guiyang 550004, China;1. Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang 330013, PR China;2. College of Service, Naval Logistics College of PLA, Tianjin 300450, PR China |
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| Abstract: | Novel series of some triazolo[4,3-b]pyridazine derivatives were designed and synthesized. All the newly synthesized compounds were evaluated for their cytotoxic activity at 10−5 M concentration towards 60 cancer cell lines according to USA NCI protocol. Most of the synthesized compounds showed good activity against SR (leukemia) cell panel. The most active compounds, 2f and 4a were subjected for further evaluation at a five dose level screening and their efficacy for c-Met kinase inhibition was determined in vitro. Binding mode of these derivatives was explored via molecular docking. |
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| Keywords: | Triazolopyridazines Pyridazines Cytotoxic activity c-Met kinase |
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