718-02-5Relevant academic research and scientific papers
Triazolopyridazine derivatives: Synthesis, cytotoxic evaluation, c-Met kinase activity and molecular docking
Ahmed, Eman M.,Khalil, Nadia A.,Taher, Azza T.,Refaey, Rana H.,Nissan, Yassin M.
, (2019/09/18)
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.
Synthesis of Some Novel 2,6-Disubstituted Pyridazin-3(2H)-one Derivatives as Analgesic, Anti-Inflammatory, and Non-Ulcerogenic Agents
Ibrahim, Tamer H.,Loksha, Yasser M.,Elshihawy, Hosam A.,Khodeer, Dina M.,Said, Mohamed M.
, (2017/09/05)
Some novel 2,6-disubstituted pyridazine-3(2H)-one derivatives were synthesized and evaluated for in vitro cyclooxygenase-2 (COX-2) inhibitory efficacy. Compounds 2-{[3-(2-methylphenoxy)-6-oxopyridazin-1(6H)-yl]methyl}-1H-isoindole-1,3(2H)-dione (5a), 2-pr
3-[(6-Arylamino)pyridazinylamino]benzoic acids: Design, synthesis and in vitro evaluation of anticancer activity
Abouzid, Khaled A. M.,Khalil, Nadia A.,Ahmed, Eman M.,Mohamed, Khaled Omar
, p. 41 - 50 (2013/03/28)
A series of novel substituted 3,6-disubstituted pyridazines based on the structure of vatalanib (PTK787) were designed and synthesized. The cytotoxicity of the final compounds was tested in vitro on HT-29 colon cancer cell line. Compounds 2a and 2b with 4-chlorophenylamino moiety, exerted the highest cytotoxic activity with IC50 values equal to 15.3 and 3.9 μM respectively. The most promising compound, 2b, was found to be about fivefold more active than vatalanib against HT-29 colon cancer cell line.
