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.

• 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

Acknowledgements

The authors are deeply thankful to the authorities of the Bioassay-Cell Culture Laboratory, Drug Discovery Unit, National Research Centre, Cairo, Egypt, for their efforts in performing the MTT cytotoxicity assay.