Journal of Pharmaceutical Sciences and Emerging Drugs has recently published an article which is related to lMethyl 6-Amino-3-acyl-4-aryl-5-cyano-4H-pyran-2-carboxylates.

lMethyl 6-Amino-3-acyl-4-aryl-5-cyano-4H-pyran-2-carboxylates, 9-aryl-12-imino-10,11dioxatricyclo-[5.3.2.01,6]-dodecan-7,8,8-tricarbonitriles, 2-R-1,2,5,6,7,8-hexahydroquinoline-3,3,4,4- tetraсarbonitriles were synthesized. The anti-proliferative activity of obtained compounds was investigated. At a concentration of 10 μM test substances activity higher than that of the drug busulfan and cisplatin showed a compounds containing in its composition fragment of ethyl 1,1,2,2-tetracarbonitrile - 2-R-1,2,5,6,7,8-hexahydroquinoline-3,3,4,4-tetraсarbonitriles.

Cancer remains one of the most serious diseases of mankind. Cancer is a leading cause of death worldwide. According to forecasts, the number of deaths from cancer in the world will continue to grow in 2030 to reach 13.1 million deaths (WHO database: Globocan, 2012). In this regard, the synthesis and investigation of antitumor activity of oxygen- and nitrogen-containing heterocyclic compounds is an urgent task for medicinal chemistry.

Despite the advent of new anticancer drugs, their clinical effectiveness is insufficient, and the spectrum of cancers that are sensitive to chemotherapy is limited. In this regard, it does not lose relevance of the question to find new chemical compounds with anti-tumour properties as the basis for further development of more effective drugs. The main criteria for the selection of the new compounds are unique chemical structure, a new mechanism of action, selective cytotoxicity availability for production, Cyano containing compounds are attracting special attention at present in the search for new antitumor agents. Thus, the cyanogenetic glucosides linamarin, lotaustralin, heterodentrin, dhurrin, amygdalin, and tetraphyllin A, which were isolated from seeds and pits of certain plants of the family Rosaceae, subfamily plum, are used in experimental oncology. Cyanogenic glucosides have been reported in more than 2,650 species of higher plants distributed over 130 families. The most famous cyanogenic glucoside is amygdalin. It was first isolated in 1830 by French chemists and has been used as an anticancer agent in Russia in 1845 . The first use of amygdalin in the United States in the treatment of cancer occurred in the early 1920s. The most promising objects are probably multifunctional heterocyclic compounds. The analysis of drugs in late development or in the market shows that 68% of them are heterocyclic hence it is not surprising that research on the synthesis of multi-functionalized heterocyclic compounds has received significant attention in the recent years.

Our researches in this area focused on the study of properties of cyanosubstituted multifunctional carbocyclic and heterocyclic compounds, derived from tetracyanoethylene , 2-arylidene malononitriles ,4-oxoalkane-1,1,2,2-tetracarbonitriles. Reactions of these compounds are usually unique and accompanied by complicated multi-step molecular level processes in simple synthesis methods.

Conclusion

The studies of the properties of 1,1,2,2-tetracyano-substituted carbocyclic and heterocyclic carbonitriles are the most promising, because we believe that this fragment is a pharmacophore alkylating mode of action. 2-R-1,2,5,6,7,8-hexahydroquinoline-3,3,4,4- tetraсarbonitriles prove to be most effective against leukaemia, lung, colon, ovarian, kidney and breast cancer.

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Journal of Pharmaceutical Sciences and Emerging Drugs
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