Novel quinolines bearing a biologically active trimethoxyphenyl moiety as a new class of antitumor agents.
The present paper describes the synthesis of some novel 2-amino-4-substituted aryl-5-oxo-1-(3,4,5-trimethoxy)-1,4,5,6,7,8-hexahydroquinoline-3-carbo-nitriles 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, 6p and 6 q showed higher activity with IC50 values 10, 10, 15 microg/mL, respectively, when compared with doxorubicin as a reference drug (IC50 value 37.5 microg/mL).
Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
Mansour S
MS
Al-Said
Mahmoud S
MS
Bashandy
Mostafa M
MM
Ghorab
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D003470:Culture Media; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D003470:Culture Media; D007202:Indicators and Reagents; D011804:Quinolines