Mediterranean Journal of Chemistry · 2019 · 10 citations · 30 references
PharmacyMedicinal ChemistryPharmacologyCancer PharmacologyDrug DiscoverySynthetic Medicinal ChemistryOncology PharmacologyStructure-activity Relationship AnalysisAnticancer ActivityAssayCancer Cell Line ModelsChemical Structure-activity RelationshipsChemical Synthesis Of AnaloguesMedicinal Chemistry ApplicationsSuzuki - Miyaura Coupling
A series of new N-aryl substituted phenyl acetamide analogs of 3-methyl-[1,2,4] triazolo[3,4-a] phthalazines were synthesized starting from commercially available, in-expensive phthalic anhydride in good yields (65-75 %) via Suzuki Coupling. These compounds were tested for inhibition activity against HCT 116 cancer cell line by using MIT assay. Among the library of compounds, N-(3-methoxyphenyl)-2-(4-(3-methyl-[1,2,4]triazolo[3,4-a]phthalazin-6-yl)phenyl) acetamide followed by 2-(4-(3-methyl-[1,2,4]triazolo[3,4-a]phthalazin-6-yl)phenyl)-N-(m-tolyl) acetamide and  N-(3-chlorophenyl)-2-(4-(3-methyl-[1,2,4]triazolo[3,4-a]phthalazin-6-yl)phenyl) acetamide  were found to be active compounds with IC50 of 70 to and 90 µg mL-1. Further, the compounds were also screened for their antimicrobial activities.
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