Publication Type : Journal Article
Publisher : J Enzyme Inhib Med Chem
Source : J Enzyme Inhib Med Chem, Volume 35, Issue 1, p.1100-1109 (2020)
Url : https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7191905/
Keywords : Antineoplastic Agents, cell proliferation, Cell Survival, Dose-Response Relationship, Drug, Drug Screening Assays, Antitumor, HCT116 Cells, Humans, Molecular Structure, Pyridazines, Structure-Activity Relationship, Tumor Cells, Cultured
Campus : Kochi
School : School of Pharmacy
Department : Pharmaceutical Chemistry & Analysis
Year : 2020
Abstract : Novel 3(2)-pyridazinone derivatives were designed, synthesised in satisfactory yields and evaluated in different experimental assays to assess their preliminary toxicity and anti-proliferative effects against HCT116 cell lines . lethality test provided LC 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 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 IC 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.
Cite this Research Publication : Z. Özdemir, Utku, S., Bijo Mathew, Carradori, S., Orlando, G., Di Simone, S., Alagöz, M. Abdullah, Özçelik, A. Berna, Uysal, M., and Ferrante, C., “Synthesis and biological evaluation of new 3(2)-pyridazinone derivatives as non-toxic anti-proliferative compounds against human colon carcinoma HCT116 cells.”, J Enzyme Inhib Med Chem, vol. 35, no. 1, pp. 1100-1109, 2020.