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Arzneimittelforschung 2011; 61(9): 527-531
DOI: 10.1055/s-0031-1296239
Antibiotics · Antimycotics · Antiparasitics · Antiviral Drugs · Chemotherapeutics · Cytostatics
Editio Cantor Verlag Aulendorf (Germany)

Novel quinolines bearing a biologically active trimethoxyphenyl moiety as a new class of antitumor agents

Mansour S. Al-Said
1   Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
,
Mahmoud S. Bashandy
2   Department of Chemistry, Faculty of Science, Al-Azhar University, Nasr City, Cairo, Egypt
,
Mostafa M. Ghorab
1   Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia
3   Department of Drug Radiation Research, National Center for Radiation Research and Technology, Nasr City, Cairo, Egypt
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Publikationsverlauf

Publikationsdatum:
03. Dezember 2011 (online)

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Abstract

The present paper describes the synthesis of some novel 2-amino-4-substituted aryl-5-oxo-1-(3,4,5-trimethoxy)-l,4,5,6,7,8-hexahydroquinoline-3-carbonitriles 6a–s starting with 3-(3,4,5-trimethoxyanilino)cyclohex-2-enone 3. All the newly synthesized compounds were evaluated for their in vitro antitumor activity. Compounds 6j, 6ρ and 6q showed higher activity with IC50 values 10, 10, 15 μg/mL, respectively, when compared with doxorubicin as a reference drug (IC50 value 37.5 μg/mL).

Key words

Antitumor activity - Cyclohexane-l,3-dione - Quinoline derivatives - Synthesis - 3,4,5-Trimethoxyaniline
 

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