Faidallah Hassan M, Saqer Alaa A, Alamry Khalid A, Khan Khalid A, Asiri Abdullah M
Department of Chemistry, Faculty of Science, King Abdulaziz University , Jeddah , Saudi Arabia and.
J Enzyme Inhib Med Chem. 2014 Jun;29(3):367-78. doi: 10.3109/14756366.2013.787421. Epub 2013 Apr 22.
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.
本研究报道了一系列新型2-氨基-3-氰基-8-甲基-4-取代-5,6,7,8-四氢喹啉以及一些衍生稠环体系的合成。十种化合物对人结肠癌HT29、肝癌HepG2和白种人乳腺腺癌MCF7细胞系显示出显著的细胞毒性活性。六种化合物表现出相当广泛的细胞毒性活性，其中两种被证明是最具活性的衍生物。同样，该系列中的七种化合物被发现具有显著的抗菌活性，其中三种被证明是最具活性的候选物。两种烷硫基嘧啶喹啉被认为是本系列中可能的抗菌和抗癌候选物。
