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Anticancer activity of newly synthesized triazolopyrimidine... 317cell line with IC 50 3.60 ± 0.39, 3.90 ± 4.20 and 4.80± 0.55 µg/mL, respectively (Table 1 and Fig. 1).The cytotoxicity of compounds 2, 3, 4, 6, 7a, 9,10, 11 and 12a was tested against lung cancer cell lineA549. For comparison, doxorubicin was also tested.All of the tested compounds except 4, 7a and 12aexhibited anticancer activity and compound 3 (IC 504.20 ± 0.50 µg/mL) was more potent than doxorubicin(IC 50 4.30 ± 0.40 µg/mL), while compound 9, 10and 2 were found to be potent near to doxorubicinwith IC 50 6.50 ± 0.67, 8.00 ± 0.83 and 8.20 ± 0.78µg/mL respectively. The order of activity was 3, 10,9, 2, 11, 6 in a descending order (Table 1 and Fig. 2).The results of colon cancer HCT116 cell linerevealed that although compounds 4, 6, 7a and 12adid not exert any activity against the cell, the rest ofcompounds 2, 3, 9, 10 and 11 had very little anticanceractivity compared to doxorubicin (IC 50 = 4.80± 0.50 µg/mL) (Table 1 and Fig. 3).In conclusion, the tested compounds exert anticarcinogenicactivity in breast MCF-7 and lung A549cancer cell lines through reducing the cell proliferationand resulted in significant growth inhibitory, especially,compounds 2, 3, 9 and 10 which revealed promisingactivity compared to the activity of the commonlyused anticancer drug, doxorubicin. The present studyreveals that MCF-7 cells are more sensitive to the testedcompounds than the other cell lines.From the above obtained results (Table 1), wecan conclude that the attachment of thioxo group atposition 2 in the triazolopyrimidine moieties resultedin an enhanced activity. It is obvious that theactivity was reduced in other derivatives which donot incorporate such functionality in their structures.Moreover, the attachment of glucosyl moiety to thetriazolopyrimidine nucleus through a thioglucosidiclinkage increased the activity. This was not the casein nearly similar structures in which the glycosylmoiety is attached to the triazolopyrimidine ringsystem through C-N linkage. In the present work,the most active compounds were the triazolopyrimidinederivatives 2, 3, 9, and 10 when compared tothe reference drug. The difference in activitybetween the compounds may be attributed to theindicated attachments to the pyrimidine ring of themolecule.AcknowledgmentThe researchers extend their appreciation to theDeanship of Scientific Research at AljoufUniversity for funding the work through theresearch group project No. 33/70.REFERENCES1. Jemal A., Siegel R., Ward E., Murray T., Xu J.,Thun M.J.: CA Cancer J. Clin. 57, 43 (2007).2. Wilhelm S., Carter C., Lynch M., Lowinger T.,Dumas J., Smith R.A., Schwartz B. et al.: Nat.Rev. Drug. Discov. 5, 835 (2006).3. Mohamed A.M., El-Sayed W.A., AlsharariM.A., Al-Qalawi H.R.M., Germoush M.O.:Arch. Pharm. Res. 36, 1055 (2013).4. Mohamed A.M., Amr A.E., Alsharari M.A., Al-Qalawi H.R.M., Germoush M.O., Al-OmarM.A.: Am. J. Biochem. Biotechnol. 7, 43(2011).5. Abd El-Salam O.I., Fahmy A.F.M., MohamedA.M., Elnaggar D.H., Hammam A.G.: World J.Chem. 5, 07 (2010).6. Hammam A.G., Abd El-Salam O.I., MohamedA.M., Abdel-Hafez A.: Indian J. Chem. 44B,1887 (2005).7. Aly A.A., Ramadan M., Mohamed A.M., EshakE.A.: J. Heterocycl. Chem. 49, 1009 (2012).8. Mohamed A.M, Alsharari M.A., Ali A.A.: J.Chem. Res. 34, 200 (2010).9. Abdel-Latif N.A., Sabry N.M., Mohamed A.M.,Abdulla M.M.: Monatsh. Chem. 138, 715(2007).10. El Ashry E.S.H., Rashed N.: Adv. Heterocycl.Chem. 71, 57 (1998).11. Fischer G.: Adv. Heterocycl. Chem. 95, 143(2008).12. Ohnishi H., Yamaguchi K., Shimada S., SuzukiY., Kumagai A.: Life Sci. 28, 1641 (1981).13. Novinson T., Springer R.H., OíBrien D.E.,Scholten M.B., Miller J.P., Robins R.K.: J.Med. Chem. 25, 420 (1982).14. Gujjar R., Marwaha A., El Mazouni F., WhiteJ., White K.L., Creason S., Shackleford D. etal.: J. Med. Chem. 52, 1864 (2009).15. Chen Q., Zhu X.L., Jiang L.L., Liu Z.M., YangG.F.: Eur. J. Med. Chem. 43, 595 (2008).16. Yu W., Goddard C., Clearfield E., Mills C.,Xiao T., Guo H., Morrey J.D. et al.: J. Med.Chem. 54, 5660 (2011).17. El-Gendy M.M.A., Shaaban M., Shaaban K.A.,El-Bondkly A.M., Laatsch H.: J. Antibiot. 61,149 (2008).18. Allen J.G., Bourbeau M.P., Wohlhieter G.E.,Bartberger M.D., Michelsen K., Hungate R.,Gadwood R.C. et al.: J. Med. Chem. 52, 7044(2009).19. Tang W., Shi D.Q.: J. Heterocycl. Chem., 47,162 (2010).