Novel All Trans-Retinoic Acid Derivatives: Cytotoxicity, Inhibition of Cell Cycle Progression and Induction of Apoptosis in Human Cancer Cell Lines

Molecules

Ebtesam Saad Al-Sheddi¹  Mai Mohammad Al-Oqail¹  Quaiser Saquib²  Maqsood Ahmed Siddiqui²  Javed Musarrat²  Abdulaziz Ali Al-Khedhairy²  Nida Nayyar Farshori¹ 

[1] Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11495, Saudi Arabia; E-Mails:;Zoology Department, College of Science, King Saud University, Riyadh 11451, Saudi Arabia; E-Mails:

关键词: all trans-retinoic acid;    anticancer activity;    apoptosis;    cell cycle arrest;    cytotoxicity;   

DOI  :  10.3390/molecules20058181

来源: mdpi

【 摘 要 】

Owing to the pharmacological potential of ATRA (all trans-retinoic acid), a series of retinamides and a 1-(retinoyl)-1,3-dicyclohexylurea compound were prepared by reacting ATRA with long chain alkyl or alkenyl fatty amines by using a 4-demethylaminopyridine (DMAP)-catalyzed N,N'-dicyclohexylcarbodiimide (DCC) coupling. The successful synthesis of the target compounds was demonstrated using a range of spectroscopic techniques. The cytotoxicity of the compounds was measured along with their ability to induce cell cycle arrest and apoptosis in human cancer cell lines MCF-7 (breast cancer) and HepG2 (liver cancer) and normal human cell line HEK293 (embryonic kidney). The results of cytotoxicity and flow cytometry data showed that the compounds had a moderate to strong effect against MCF-7 and HepG2 cells and were less toxic to HEK293 cells. N-oleyl-retinamide was found to be the most potent anticancer agent and was more effective against MCF-7 cells than HepG2 cells.

【 授权许可】

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© 2015 by the authors; licensee MDPI, Basel, Switzerland.