title: Synthesis, antimicrobial and anticancer activities of a novel series of diphenyl 1-(pyridin-3-yl)ethylphosphonates.
abstract: A novel series of diphenyl 1-(arylamino)-1-(pyridin-3-yl)ethylphosphonates 1-5 was obtained in high yields from reactions of 3-acetyl pyridine with aromatic amines and triphenylphosphite in the presence of lithium perchlorate as a catalyst. The structures of the synthesized compounds were confirmed by IR, (1)H NMR spectral data and microanalyses. Compounds 1-5 showed high antimicrobial activities against Escherichia coli (NCIM2065) as a Gram-negative bacterium, Bacillus subtilis (PC1219) and Staphylococcus aureus (ATCC25292) as Gram-positive bacteria and Candidaalbicans and Saccharomyces cerevisiae as fungi, at low concentrations (10-100 μg/mL). Also, the synthesized compounds showed significant cytotoxicity anticancer activities against liver carcinoma cell line (HepG2) and human breast adenocarcinoma cell line (MCF7). The lethal dose of the synthesized compounds was also determined and indicated that most compounds are safe to use.
authors.affiliation: Department of Chemistry, Faculty of Science, Tanta University, Tanta 31527, Egypt.
authors.forename: Mohamed F
authors.initials: MF
authors.lastname: Abdel-Megeed
authors.forename: Badr E
authors.initials: BE
authors.lastname: Badr
authors.forename: Mohamed M
authors.initials: MM
authors.lastname: Azaam
authors.forename: Gamal A
authors.initials: GA
authors.lastname: El-Hiti
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D005658:Fungi / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D056945:Hep G2 Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D063065:Organophosphonates / Q000737:chemistry / Q000494:pharmacology; D010757:Phosphorous Acids / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000737:chemistry
chemical_list: D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D063065:Organophosphonates; D010757:Phosphorous Acids; D011725:Pyridines; C570063:phosphonic acid; C023666:pyridine