<abstract xmlns="http://www.w3.org/1999/xhtml">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-1). Also, compounds 5, 8 and 10 were found nearly as active as doxorubicin (IC50 28.85, 23.48 and 27.51 μmol L-1).</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-1). Also, compounds 5, 8 and 10 were found nearly as active as doxorubicin (IC50 28.85, 23.48 and 27.51 μmol L-1).

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

Department of Pharmacognosy College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Kingdom of Saudi Arabia

Department of Drug Radiation Research, National Center for Radiation Research and Technology Atomic Energy, Authority, P.O.Box 29 Nasr City, Cairo, Egypt

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

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

A novel series of thiophenes having biologically active sulfonamide 2-11, 3-methylisoxazole 12, 4-methoxybenzo[d] thiazole 13, quinoline 14, 15,...

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

Publicado en línea: 20 dic 2014

Páginas: 419 - 431

Aceptado: 03 jul 2014

DOI: https://doi.org/10.2478/acph-2014-0035

Palabras clave
thiophenes, sulfonamides, isoxazole, benzothiazole, quinoline, anthracene, anticancer activity

© by Mostafa M. Ghorab

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

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

Publicado en línea: 20 dic 2014

Páginas: 419 - 431

Aceptado: 03 jul 2014

DOI: https://doi.org/10.2478/acph-2014-0035

Palabras clavethiophenes, sulfonamides, isoxazole, benzothiazole, quinoline, anthracene, anticancer activity

© by Mostafa M. Ghorab

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Palabras clave
thiophenes, sulfonamides, isoxazole, benzothiazole, quinoline, anthracene, anticancer activity