Al-Said Mansour S, Ghorab Mostafa M, Nissan Yassin M
Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, 2457, Riyadh, 11451, Saudi Arabia.
Chem Cent J. 2012 Jul 2;6(1):64. doi: 10.1186/1752-153X-6-64.
Several new sulfonebiscompounds having a biologically active 1,2-dihydropyridine-2-one 3-19, acrylamide 20, chromene 21, 22 and chromenopyridine 23, 24 moieties were synthesized and evaluated as potential anticancer agents. The structures of the products were confirmed via elemental analyses and spectral data. The screening tests showed that many of the biscompounds obtained exhibited good anticancer activity against human breast cell line (MCF7) comparable to doxorubicin which was used as reference drug. Compounds 11, 17 and 24 showed IC50 values 35.40 μM, 29.86 μM and 30.99 μM, respectively. In order to elucidate the mechanism of action of the synthesized compounds as anticancer agents, docking on the active site of farnesyltransferase and arginine methyltransferase was also performed and good results were obtained.
合成了几种具有生物活性的1,2 - 二氢吡啶 - 2 - 酮3 - 19、丙烯酰胺20、色烯21、22以及色烯吡啶23、24部分的新型砜双化合物,并将其作为潜在的抗癌剂进行了评估。通过元素分析和光谱数据确认了产物的结构。筛选试验表明,所获得的许多双化合物对人乳腺癌细胞系(MCF7)表现出良好的抗癌活性,与用作参考药物的阿霉素相当。化合物11、17和24的IC50值分别为35.40 μM、29.86 μM和30.99 μM。为了阐明合成化合物作为抗癌剂的作用机制,还对法尼基转移酶和精氨酸甲基转移酶的活性位点进行了对接,并获得了良好的结果。