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

被引:66
作者
Ghorab, Mostafa M. [1 ,2 ]
Bashandy, Mahmoud S. [3 ]
Alsaid, Mansour S. [1 ]
机构
[1] King Saud Univ, Coll Pharm, Dept Pharmacognosy, Riyadh 11451, Saudi Arabia
[2] Natl Ctr Radiat Res & Technol Atom Energy, Dept Drug Radiat Res, Cairo, Egypt
[3] Al Azhar Univ, Fac Sci Boys, Dept Chem, Cairo, Egypt
关键词
thiophenes; sulfonamides; isoxazole; benzothiazole; quinoline; anthracene; anticancer activity; CARBONIC-ANHYDRASE; BEARING; ANTIBACTERIAL; INHIBITORS; COMPLEXES; DESIGN;
D O I
10.2478/acph-2014-0035
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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 mu mol L-1) revealed higher cytotoxic activities than that of doxorubicin (IC50 = 32.00 mu mol L-1). Also, compounds 5, 8 and 10 were found nearly as active as doxorubicin (IC50 28.85, 23.48 and 27.51 mu mol L-1).
引用
收藏
页码:419 / 431
页数:13
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