<abstract xmlns="http://www.w3.org/1999/xhtml"><p> Novel nineteen compounds based on a 4-aminoquinoline scaffold were designed and synthesized as potential antiproliferative agents. The new compounds were N-substituted at the 4-position by aryl or heteroaryl (1-9), quinolin- 3-yl (10), 2-methylquinolin-3-yl (11), thiazol-2-yl (12), and dapsone moieties (13, 14 and 18). Bis-compounds 15, 16 and 19 were also synthesized to assess their biological activity. All the newly synthesized comounds were tested for in vitro antiproliferative activity against the MCF-7 breast cancer cell line. Seventeen of the novel compounds showed higher activity than the reference drug doxorubicin. The corresponding 7-(trifluoromethyl)-N-(3,4,5-trimethoxyphenyl)quinolin-4- amine 1, N-(7-(trifluoromethyl)quinolin-4-yl)quinolin- 3- amine (10), 2-methyl-N-(7-trifluorome-thyl)quinolin-4-yl) quinolin-3-amine (11) and N-(4-(4-aminophenylsulfonyl) phenyl)-7-chloroquinolin-4-amine (13) were almost twice to thrice as potent as doxorubicin. Biological screening of the tested compounds could offer an encouraging framework in this field that may lead to the discovery of potent anticancer agents.</p></abstract>

Novel nineteen compounds based on a 4-aminoquinoline scaffold were designed and synthesized as potential antiproliferative agents. The new compounds were N-substituted at the 4-position by aryl or heteroaryl (1-9), quinolin- 3-yl (10), 2-methylquinolin-3-yl (11), thiazol-2-yl (12), and dapsone moieties (13, 14 and 18). Bis-compounds 15, 16 and 19 were also synthesized to assess their biological activity. All the newly synthesized comounds were tested for in vitro antiproliferative activity against the MCF-7 breast cancer cell line. Seventeen of the novel compounds showed higher activity than the reference drug doxorubicin. The corresponding 7-(trifluoromethyl)-N-(3,4,5-trimethoxyphenyl)quinolin-4- amine 1, N-(7-(trifluoromethyl)quinolin-4-yl)quinolin- 3- amine (10), 2-methyl-N-(7-trifluorome-thyl)quinolin-4-yl) quinolin-3-amine (11) and N-(4-(4-aminophenylsulfonyl) phenyl)-7-chloroquinolin-4-amine (13) were almost twice to thrice as potent as doxorubicin. Biological screening of the tested compounds could offer an encouraging framework in this field that may lead to the discovery of potent anticancer agents.

Design, Synthesis and Potential Anti-Proliferative Activity of Some Novel 4-Aminoquinoline Derivatives

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

Pharmaceutical Chemistry Department, Faculty of Pharmacy Cairo University, Cairo, Egypt

Acta Pharmaceutica

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

Novel nineteen compounds based on a 4-aminoquinoline scaffold were designed and synthesized as potential antiproliferative agents. The new compounds were...

Design, Synthesis and Potential Anti-Proliferative Activity of Some Novel 4-Aminoquinoline Derivatives

Published Online: Oct 08, 2014

Page range: 285 - 297

Accepted: May 20, 2014

DOI: https://doi.org/10.2478/acph-2014-0030

Keywords
4-aminoquinolines, bis-compounds, dapsone, antiproliferative activity

© by Mostafa M. Ghorab

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

Design, Synthesis and Potential Anti-Proliferative Activity of Some Novel 4-Aminoquinoline Derivatives

Published Online: Oct 08, 2014

Page range: 285 - 297

Accepted: May 20, 2014

DOI: https://doi.org/10.2478/acph-2014-0030

Keywords4-aminoquinolines, bis-compounds, dapsone, antiproliferative activity

© by Mostafa M. Ghorab

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

Keywords
4-aminoquinolines, bis-compounds, dapsone, antiproliferative activity