Dapson in heterocyclic chemistry, part VIII: synthesis, molecular docking and anticancer activity of some novel sulfonylbiscompounds carrying biologically active 1,3-dihydropyridine, chromene and chromenopyridine moieties

Chemistry Central Journal

Mansour S Al-Said²  Mostafa M Ghorab²  Yassin M Nissan¹ 

[1] Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt

[2] Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, 2457, Riyadh, 11451, Saudi Arabia

关键词: Anticancer activity;    Pyridnochromenes;    Chromenes;    Pyridines;    Sulfone;   

Others  :  788112
DOI  :  10.1186/1752-153X-6-64

 received in 2012-04-14, accepted in 2012-06-07,  发布年份 2012

【 摘 要 】

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.

【 授权许可】

   
2012 Al-Said et al; licensee Chemistry Central Ltd.

【 图 表 】

Scheme 1

Scheme 2

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Scheme 4

Figure 1.

Figure 2.

Figure 3.

Figure 4.

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