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Synthesis and biological evaluation of new 3(2H)-pyridazinone derivatives as non-toxic anti-proliferative compounds against human colon carcinoma HCT116 cellsÖzdemir, ZeynepUtku, SemraMathew, BijoCarradori, SimoneOrlando, GiustinoDi Simone, SimonettaAlagöz, Mehmet AbdullahÖzçelik, Azime BernaUysal, MehtapFerrante, Claudioanti-proliferative agentsArtemia salina lethality testHCT116kynurenic acidpyridazinoneSerotoninwound healingAntineoplastic AgentsCell ProliferationCell SurvivalDose-Response Relationship, DrugDrug Screening Assays, AntitumorHCT116 CellsHumansMolecular StructurePyridazinesStructure-Activity RelationshipTumor Cells, Culturedantimitotic agentdaunorubicinn' (2 bromobenzylidene) 2 [3 (3 fluoro 4 methoxyphenyl) 6 oxopyridazin 1(6h) yl]acetohydraziden' (2 fluorobenzylidene) 2 [3 (3 fluoro 4 methoxyphenyl) 6 oxopyridazin 1(6h) yl]acetohydraziden' (2 methoxybenzylidene) 2 [3 (3 fluoro 4 methoxyphenyl) 6 oxopyridazin 1(6h) yl]acetohydraziden' (2 methylbenzylidene) 2 [3 (3 fluoro 4 methoxyphenyl) 6 oxopyridazin 1(6h) yl]acetohydraziden' (2,4 dichlorobenzylidene) 2 [3 (3 fluoro 4 methoxyphenyl) 6 oxopyridazin 1(6h) yl]acetohydraziden' (4 bromobenzylidene) 2 [3 (3 fluoro 4 methoxyphenyl) 6 oxopyridazin 1(6h) yl]acetohydraziden' (4 fluorobenzylidene) 2 [3 (3 fluoro 4 methoxyphenyl) 6 oxopyridazin 1(6h) yl]acetohydraziden' (4 hydroxybenzylidene) 2 [3 (3 fluoro 4 methoxyphenyl) 6 oxopyridazin 1(6h) yl]acetohydraziden' (4 isopropylbenzylidene) 2 [3 (3 fluoro 4 methoxyphenyl) 6 oxopyridazin 1(6h) yl]acetohydraziden' (4 methoxybenzylidene) 2 [3 (3 fluoro 4 methoxyphenyl) 6 oxopyridazin 1(6h) yl]acetohydrazideNovel 3(2H)-pyridazinone derivatives were designed, synthesised in satisfactory yields and evaluated in different experimental assays to assess their preliminary toxicity in vivo and anti-proliferative effects against HCT116 cell lines in vitro. Artemia salina lethality test provided LC50 values >100 µg/mL for all compounds. Successive assays revealed that some compounds were endowed with a promising anti-proliferative effect against HCT116 cells, alone or stimulated by serotonin as a pro-inflammatory factor in order to mimick an inflamed model in vivo of cancer cell microenvironment. Moreover, the kinurenic acid level after treatment with these newly synthesised compounds was monitored as a marker of anti-proliferation in colon carcinoma models. The IC50 values obtained for the best-in-class compounds were comparable to that of daunorubicin as a reference drug. Conversely, these compounds were not able to counteract the spontaneous migration of human cancer HCT116 cell line in the wound healing paradigm. © 2020, © 2020 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group.Taylor and Francis Ltd2020Articlehttps://rdlopen.rawdatalibrary.net/r/ebyu/13649https://doi.org/10.1080/14756366.2020.17556701475-6366enJournal of Enzyme Inhibition and Medicinal Chemistryinfo:eu-repo/semantics/openAccessinfo:eu-repo/semantics/articlehttps://ebyu-rdlopen.rawdatalibrary.net/tr/items/ebyu/13649