Click synthesis of new 7-chloroquinoline derivatives by using ultrasound irradiation and evaluation of their biological activity

[摘要] This study describes the click synthesis of new 7-chloroquinoline derivatives by using ultrasound irradiation and evaluation of their activity as antimicrobial, antimalarial and the anticancer. All the compounds show moderate antimalarial activity with IC50 < 100 μM, six of them showed high antimalarial activity (2, 3, 4, 6, 8 and 9) with IC50 < 50 μM. The most active 7-chloroquinoline derivative is a compound (9). Also, the newly synthesized compounds were screened for their antitumor activity towards three lines of cancer cells, MCF-7 (human breast cancer), HCT-116 (colon carcinoma) and Hela (Cervical carcinoma) cell lines. Compounds (3) and (9) exerted the highest activity on all cell lines and showed special selectivity toward MCF-7 cells and the antibacterial screening data showed moderate to good inhibition zone (12.5 ± 0.63–23.8 ± 1.5) towards all the tested compounds. Elucidation of the structures of these new pure compounds was based on, IR, 1H NMR, 13C NMR, MS and their elemental analysis.

[学科分类] 化学（综合）

[关键词] Ultrasonic radiation;7-chloroquinoline;click chemistry;antimalarial activity;and cytotoxicity