Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Eur J Med Chem. 2010 May;45(5):1849-53. doi: 10.1016/j.ejmech.2010.01.022. Epub 2010 Jan 20.
The present article describes the synthesis of some novel 4-(2-amino-3-cyano-4-(substituted-aryl)-5-oxo-5,6,7,8-tetrahydroquinolin-1(4H)-yl)benzenesulfonamide (23-41) starting with 4-(3-oxo-cyclohex-1-enylamino)benzenesulfonamide (3). All the newly synthesized compounds were evaluated for their in vitro antitumor activity. Compounds 32, 25, 41, 35, 33, and 37 with IC50 values (2.5, 3, 5, 10, 12, and 12.5 microg/mL) are more potent and efficacious than Doxorubicin (CAS-23214-92-8) as reference drug with (IC50 value=37.5 microg/mL). Also, compounds 28, 30, 31, and 34 (with IC50 values=25 microg/mL) are nearly as active as Doxorubicin.
本文描述了一些新型 4-(2-氨基-3-氰基-4-(取代芳基)-5-氧代-5,6,7,8-四氢喹啉-1(4H)-基)苯磺酰胺 (23-41) 的合成，起始原料为 4-(3-氧代环己-1-烯基氨基)苯磺酰胺 (3)。所有新合成的化合物都进行了体外抗肿瘤活性评估。化合物 32、25、41、35、33 和 37 的 IC50 值（2.5、3、5、10、12 和 12.5 μg/mL）比作为参考药物的多柔比星（CAS-23214-92-8）更有效，其 IC50 值为 37.5 μg/mL。此外，化合物 28、30、31 和 34（IC50 值为 25 μg/mL）与多柔比星相当有效。
