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Journal of Chemistry
Volume 2014, Article ID 126323, 8 pages
Research Article

Synthesis of 1,8-Naphthyridine Derivatives under Ultrasound Irradiation and Cytotoxic Activity against HepG2 Cell Lines

1Chemistry Department, Faculty of Science, King Abdulaziz University, P.O. Box 80203, Jeddah 21589, Saudi Arabia
2Medicinal Chemistry Department, National Research Center, Dokki, Cairo 12622, Egypt

Received 4 December 2013; Revised 27 January 2014; Accepted 27 January 2014; Published 12 March 2014

Academic Editor: Angelo de Fatima

Copyright © 2014 N. S. Ahmed et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


Novel pyrazole derivatives 3a,b, 5, 1,3,4-oxadiazole 6, 1,3,4-thiadiazole 8, and 1,2,4-triazole 9a–c incorporated into 1,8-naphthyridine have been synthesized using the versatile synthon 2-(2,7-dimethyl-1,8-naphthyridin-4-yloxy) acetohydrazide 1. An improvement in rates and yields was observed when the reactions were carried out under ultrasonic irradiation compared with the classical synthesis. The newly synthesized compounds were evaluated for HepG2 cell growth inhibition. The results obtained revealed that the tested compounds possess inhibitory effect on the growth of HepG2 liver cancer cells. The results were compared to doxorubicin (DOX) as a reference drug (IC50 : 0.04  M). Compounds 9b showed the highest inhibition activity against HepG2 cell line (IC50 : 0.048  M) among all tested compounds.