Original scientific paper

https://doi.org/10.2478/acph-2014-0033

Novel thiophene derivatives with sulfonamide, isoxazole, benzothiazole, quinoline and anthracene moieties as potential anticancer agents

MOSTAFA M. GHORAB ; Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Kingdom of Saudi Arabia; Deprtment of Drug Radiation Research, National Center for Radiation Research And Technology, Atomic Energy, Authority, P.O.Box 2
MAHMOUD S. BASHANDY ; Department of Chemistry, Faculty of Science (Boy's) , Al-Azhar University, Nasr City, Cairo, Egypt; Department of Chemistry, University College at Al-Jomoom, Umm Al-Qura University, 2026, Makkah, Saudi Arabia
MANSOUR S. AL-SAID ; Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Kingdom of Saudi Arabia

Abstract

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

Hrčak ID:

123213

URI

https://hrcak.srce.hr/123213

Publication date:

31.12.2014.

Visits: 3.141 *