Design,synthesis And In Vitro Antitumor Activity Of Aromatic Alkylamine Compounds

Cancer is a serious factor affecting human health and it is one of the diseases that is currently the most common and difficult to cure.In recent years,the prevalence of cancer worldwide is continued to growing.Compared to IARC released the 2012 global cancer database in the Chinese cancer data,the situation has become more severe.Cancer has become an important factor in the current impacting on human health.At present,the treatment of cancer to the main chemoterapy,but the market mainstream anti-cancer drugs are generally toxic side effects or expensive.To develope of new anti-tumor drugs is the urgent problem to be solved.Voltage-Gated Sodium Channels(VGSCs)act as a novel channel protein receptor,it is usually expressed in excitable cells(such as nerves,muscle cells,etc.).In recent years,many studies have shown that VGSCs can be expressed in metastatic tumor cells(such as cervical cancer,prostate cancer,breast cancer,lung cancer,etc.).It plays an important physiological role in invasion and metastasis and is the excitement of tissue action potential of the key ions aisle.VGSCs has become a hot research topic for new antitumor drugs in recent years.Since the first VGSCs blocker tetrodotoxin(TTX)has been isolated,hundreds of VGSCs blockade compounds have been reported.Compound T1 and T2 were synthesized by the reaction of 1,1'-(4-chlorobutylidene)bis(4-flourobenzene)by Gabriel,hydrazinolysis,coupling and reduction reaction.Compounds T3~T11 were synthesized in similar method to the use of DMSO as a solvent through a series of coupling reaction.The method has the advantages of simple synthesis,mild reaction conditions and few synthesis steps.All of the compounds of this study were confirmed by1H-NMR,13C-NMR and MS.Biological evaluation in vitro were evaluated by human prostate cancer cells(DU145,PC3),breast cancer cells(MCF-7,MDB-MB-231,MDB-MB-453)and 926 by MTT assay.Compound T5 and T7 have good antitumor activity and low toxicity among the compounds,with a certain degree of innovation,for the new anti-tumor drug design has laid a foundation.