Russian Journal of General Chemistry

, Volume 88, Issue 11, pp 2394–2399 | Cite as

Synthesis and Evaluation of Anticancer Activity of Indazole Derivatives

  • G. Sandeep ReddyEmail author
  • S. Mohanty
  • J. Kumar
  • B. Venteswar Rao


A novel series of indazole 13a13j derivatives has been synthesized. Their structures are confirmed by 1H and 13C NMR, and mass spectral analysis. The compounds are tested for their anticancer activity against four human cancer cell lines including A549 (Lung), MCF7 (Breast), A375 (Melanoma), and HT-29 (Colon), using combretastatin-A4 as a positive control. Most of the synthesized compounds demonstrate potent activity against the above cell lines. Here IC50 values of target compounds range from 0.010±0.0042 to 12.8±3.77 μM and the control drug from 0.11±0.02 to 0.93±0.034 μM. The compounds 13a, 13b, 13e, 13g, 13h, and 13j are determined to be more potent than the positive control.


indazole pazopanib granisetron 2-aminobenzothiazole anticancer activity 


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. 1.(a)
    Cerecetto, H., Gerpe, A., Gonzalez, M., Aran, V. J., and de Ocariz, C.O., Mini-Rev. Med. Chem., 2005, vol. 5, p. 869. doi 10.2174/138955705774329564CrossRefGoogle Scholar
  2. (b).
    Schmidt, A., Beutler, A., and Snovydovych, B., Eur. J. Org. Chem., 2008, p. 4073. doi 10.1002/ejoc.200800227Google Scholar
  3. 2.
    Maggio, B., Raimondi, M.V., Raffa, D., Plescia, F., Cascioferro, S., Plescia, S., Tolomeo, M., Di Cristina, A., Pipitone, R.M., Grimaudo, S., and Daidone, G., Eur. J. Med. Chem., 2011, vol. 46, p. 168. doi 10.1016/j.ejmech.2010.10.032CrossRefGoogle Scholar
  4. 3.
    Giorgio, G., Palazzo, G., Germani, C., Barcellona, P.S., and Silvestrini, B., J. Med. Chem., 1976, vol. 19, p. 778. doi 10.1021/jm00228a008CrossRefGoogle Scholar
  5. 4.
    Upadhyay, A., Srivastava, S., and Yadav, R., Ind. J. Chem., 2011, vol. 50, p.89.Google Scholar
  6. 5.
    Salvatore, P., Demetrio, R., Fabiana, P., Casula, G., Maggio, B., Daidone, G., Raimondi, M.V., Cusimano, M.G., Bombieri, G., and Meneghetti, F., ARKIVOC, 2010, vol. 2010 (x), p.163.Google Scholar
  7. 6.
    Rodgers, J.D., Johnson, B.L., Wang, H., Greenberg, R.A., Erickson-Viitanen, S., Klabe, R.M., Cordova, B.C., Rayner, M.M., Lam, G.N., and Chang, C.-H., Bioorg. Med. Chem Lett., 1996, vol. 6, p. 2919. doi 10.1016/S0960-894X(96)00531-8CrossRefGoogle Scholar
  8. 7.
    Huang, S.T., Hsei, I.J., and Chen, C., Bioorg. Med. Chem., 2006, vol. 14, p. 6106. doi 10.1016/j.bmc.2006.05.007CrossRefGoogle Scholar
  9. 8.
    Gurupadayya, B.M., Gopal, M., Padmashali, B., and Vaidya, V.P., Ind. J. Heterocy Chem., 2005, vol. 15, p.169.Google Scholar
  10. 9.
    Akhtar, T., Hameed, S., Al-Masoudi, N., Loddo, R., and Colla, P., Acta Pharm., 2008, vol. 58, p. 135. doi 10.2478/v10007-008-0007-2CrossRefGoogle Scholar
  11. 10.
    Suresh, C.H., Rao, J.V., Jayaveera, K.N., and Subudhi, S.K., Int. J. Pharm., 2013, vol. 2, p.257.Google Scholar
  12. 11.
    Siddiqui, N., Pandeya, S.N., Khau, S.A., Stables, J., Rana, A., Alam, M., MdArshad, F., and Bhat, M.A., Bioorg. Med. Chem., 2007, vol. 17, p. 255. doi 10.1016/j.bmcl.2006.09.053CrossRefGoogle Scholar
  13. 12.
    Palmer, F.J., Trigg, R.B., and Warrington, J.V., J. Med. Chem., 1971, vol. 14, p. 248. doi 10.1021/jm00285a022CrossRefGoogle Scholar
  14. 13.
    Pattan, S.R., Suresh, Ch., Pujar, V.D., Reddy, V.V.K., Rasal, V.P., and Koti, B.C., Ind. J. Chem., 2005, vol. 44B, p. 2404.Google Scholar
  15. 14.
    Singh, M., Singh, S.K., Gangwar, M., Nath, G., and Singh, S.K., RSC Adv., 2014, vol. 4, p. 19013. doi 10.1039/C4RA02649GCrossRefGoogle Scholar
  16. 15.
    Peters, A.T., and Yang, S.S., Dyes Pigments, 1995, vol. 28, p. 151. doi 10.1016/0143-7208(95)00012-5CrossRefGoogle Scholar

Copyright information

© Pleiades Publishing, Ltd. 2018

Authors and Affiliations

  • G. Sandeep Reddy
    • 1
    Email author
  • S. Mohanty
    • 2
  • J. Kumar
    • 1
  • B. Venteswar Rao
    • 1
  1. 1.Organic Chemistry and Chemistry of FoodsDrugs and Water Analysis Andhra UniversityVisakhapatnamIndia
  2. 2.Process Research and DevelopmentDr. Reddy’s Laboratories Limited, API Plant, IDA BollaramHyderabad, TelanganaIndia

Personalised recommendations