title: Synthesis and biological evaluation of some novel tetrahydroquinolines as anticancer and antimicrobial agents.
abstract: This study reports the synthesis of a series of new 2-amino-3-cyano-8-methyl-4-substituted-5,6,7,8-tetrahydroquinolines along with some derived fused-ring systems. Ten compounds have shown remarkable cytotoxic activity against human colon carcinoma HT29, hepatocellular carcinoma HepG2 and Caucasian breast adenocarcinoma MCF7 cell lines. Six compounds showed considerable broad-spectrum cytotoxic activity among which two proved to be the most active derivatives. Likewise, seven compounds from the series were found to exhibit significant antimicrobial activity and three of them proved to be the most active candidates. Two alkylthio-pyrimido quinolines are suggested as possible antimicrobial and anticancer candidates in the present series.
authors.affiliation: Department of Chemistry, Faculty of Science, King Abdulaziz University , Jeddah , Saudi Arabia and.
authors.forename: Hassan M
authors.initials: HM
authors.lastname: Faidallah
authors.forename: Alaa A
authors.initials: AA
authors.lastname: Saqer
authors.forename: Khalid A
authors.initials: KA
authors.lastname: Alamry
authors.forename: Khalid A
authors.initials: KA
authors.lastname: Khan
authors.forename: Abdullah M
authors.initials: AM
authors.lastname: Asiri
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001234:Aspergillus niger / Q000187:drug effects / Q000254:growth & development; D002176:Candida albicans / Q000187:drug effects / Q000254:growth & development; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000187:drug effects / Q000254:growth & development; D006094:Gram-Positive Bacteria / Q000187:drug effects / Q000254:growth & development; D019073:HT29 Cells; D056945:Hep G2 Cells; D006801:Humans; D061986:MCF-7 Cells; D021281:Quantitative Structure-Activity Relationship; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D011804:Quinolines
keywords: 2-Amino-3-cyano-8-methyl-4-substituted-5,6,7,8-tetrahydroquinolines; 3H-pyrimido[4,5-b]quinolin-4-ones; antimicrobial agents; cytotoxic agents