Synthesis, Anticancer Activity, and Molecular Docking of New Furan-2-one and Pyrazole heterocycles Based on 5,6,7,8-Tetrahydronaphthalene

Document Type : Original Article


1 applied organic chemistry , nrc

2 Tanning Materials and Leather Technology Department, National Research Centre, Egypt

3 Bioinformatics Department, Armed Forces College of Medicine (AFCM) Cairo, Egypt

4 Applied Organic Chemistry Department, Chemical Industries Research Institute, National Research Center, Dokki, Giza, 12622 Egypt;


Novel furan-2-one and pyrazole heterocycles incorporating 5,6,7,8-tetrahydronaphthalene moiety 4, 8, 10a-c, 12a-c and 13 were prepared starting from 2-acetyl tetralin via reaction with diethyl oxalate followed by cyclization using hydroxylamine hydrochloride, and hydrazine hydrate. Further treatment of carbohydrazide 8 with isatin derivatives 9a-c and hydrazonoyl halides 11a-c afforded N'-(5-subs.-2-oxoindolin-3-ylidene)-3-(5,6,7,8-tetrahydronaphthalen-2-yl)-1H-pyrazole-5-carbohydrazides 10a-c and N'-aryl-2-(2-(3-(5,6,7,8-tetrahydronaphthalen-2-yl)-1H-pyrazole-5-carbonyl)hydrazono)propanehydrazonoyl chlorides 12a-c. The novel compounds were examined in vitro for their anti-tumor activities against HepG-2 and MCF-7 human carcinoma cell lines using MTT assay. Most compounds showed good to moderate activities against HepG-2 carcinoma cells and HepG-2 cells.


Main Subjects