title: 3-cyano-8-methyl-2-oxo-1,4-disubstituted-1,2,5,6,7,8-hexahydroquinolines: synthesis and biological evaluation as antimicrobial and cytotoxic agents.
abstract: The synthesis, in vitro antimicrobial and cytotoxic activities of some novel hexahydroquinolines supported with various pharmacophores are described. The results revealed that 18 compounds displayed pronounced activity against Staphylococcus aureus and Escherichia coli bacteria beside a moderate antifungal activity. Compound 25 is the most active candidate with equipotency to ampicillin against S. aureus, E. coli and Pseudomonas aeruginosa, together with an obvious antifungal activity. Additionally, 12 compounds showed remarkable cytotoxic efficiency against human colon carcinoma HT29, hepatocellular carcinoma Hep-G2 and Caucasian breast adenocarcinoma MCF7 cell lines. Among these, the analogs 22 and 25 proved to be the most active cytotoxic members. Collectively, the results would suggest that compounds 22 and 25 could be considered as possible dual antimicrobial-anticancer agents.
authors.affiliation: Department of Chemistry, Faculty of Science, King Abdulaziz University, Jeddah, Saudi Arabia.
authors.forename: Hassan M
authors.initials: HM
authors.lastname: Faidallah
authors.forename: Sherif A F
authors.initials: SA
authors.lastname: Rostom
authors.forename: Abdullah M
authors.initials: AM
authors.lastname: Asiri
authors.forename: Khalid A
authors.initials: KA
authors.lastname: Khan
authors.forename: Mohammed F
authors.initials: MF
authors.lastname: Radwan
authors.forename: Hani Z
authors.initials: HZ
authors.lastname: Asfour
mesh_terms: D000230:Adenocarcinoma / Q000188:drug therapy / Q000473:pathology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology; D006528:Carcinoma, Hepatocellular / Q000188:drug therapy / Q000473:pathology; D045744:Cell Line, Tumor; D060326:Chemistry Techniques, Synthetic; D003603:Cytotoxins / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004354:Drug Screening Assays, Antitumor; D004926:Escherichia coli / Q000187:drug effects; D019073:HT29 Cells / Q000187:drug effects; D006801:Humans; D006912:Hydroxyquinolines / Q000737:chemistry*; D008113:Liver Neoplasms / Q000188:drug therapy / Q000473:pathology; D008826:Microbial Sensitivity Tests; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D000935:Antifungal Agents; D000970:Antineoplastic Agents; D003603:Cytotoxins; D006912:Hydroxyquinolines