1421471-44-4Relevant articles and documents
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
Faidallah, Hassan M.,Rostom, Sherif A. F.,Asiri, Abdullah M.,Khan, Khalid A.,Radwan, Mohammed F.,Asfour, Hani Z.
, p. 123 - 130 (2013)
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.
Design, synthesis and biological evaluation of some novel hexahydroquinoline-3-carbonitriles as anticancer and antimicrobial agents
Faidallah, Hassan M.,Saqer, Alaa A.,Alamry, Khalid A.,Khan, Khalid A.,Zayed, Mohie A. M.,Khan, Salman A.
, p. 8139 - 8144 (2015/02/02)
The synthesis of ten novel 3-cyano-8-methyl-2-oxo-1,4-disubstituted-1,2,5,6,7,8-hexahydro-quinolines supported with benzensulfonyl and phenylthiocarbamoyl pharmacophores that are known to contribute to potential chemotherapeutic effects is described. They were evaluated in vitro for their antimicrobial activity against eight different microorganisms and for their cytotoxic effects against three different human tumor cell lines. The results revealed that nine compounds displayed variable inhibitory effects on the growth of the tested Gram-positive and Gram-negative bacteria with special pronounced activity against S. aureus and E. coli bacterial strains, in addition to a moderate antifungal activity against C. albicans. On the other hand, six compounds were able show remarkable cytotoxic efficiency against human colon carcinoma HT29, hepatocellular carcinoma Hep-G2 and Caucasian breast adenocarcinoma MCF7 cell lines. Collectively, the results would suggest that compounds 15 and 16 could be considered as possible dual antimicrobial-anticancer agents.
