Acta Pharm. 64 (2014) 419-431
Original research paper
Novel
thiophene derivatives with sulfonamide, isoxazole, benzothiazole, quinoline and
anthracene moieties as potential anticancer agents
MOSTAFA M. GHORAB, MAHMOUD S. BASHANDY and MANSOUR S. AL-SAID
1 Department of
Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457,
Riyadh 11451, Kingdom of Saudi Arabia
2 Department of Drug Radiation Research, National
Center for Radiation Research and Technology, Atomic Energy Authority, P.O.Box
29, Nasr City, Cairo, Egypt
3 Department of Chemistry, Faculty of Science (Boy's), Al-Azhar University,
Nasr City, Cairo, Egypt
4 Department of
Chemistry,
Accepted July 3, 2014
A novel series of thiophenes having biologically active sulfonamide (2-11), 3-methylisoxazole (12), 4-methoxybenzo[d]thiazole (13), quinoline (14, 15), benzoylphenylamino (16) and anthracene-9,10-dione (17) moieties were prepared. Structures of the newly synthesized compounds were established by elemental analysis and spectral data. All newly synthesized compounds were evaluated for their in vitro anticancer activity against human breast cancer cell line (MCF7). Most of the screened compounds showed cytotoxic activities compared to doxorubicin as a positive control. Compounds 6, 7, 9 and 13 (IC50 values 10.25, 9.70, 9.55 and 9.39 µmol L–1 revealed higher cytotoxic activities than that of doxorubicin (IC50 = 32.00 µmol L). Also, compounds 5, 8 and 10 were found nearly as active as doxorubicin (IC50 values 28.85, 23.48 and 27.51 µmol L–1).
Keywords: thiophenes, sulfonamides, isoxazole, benzothiazole,
quinoline, anthracene, anticancer activity
