Synthesis and Anti-Proliferative Activity of Novel Tricyclic Compounds Derived from 2-Substituted 1,3-Indandione


A new series of fused 1,3-indandione derivatives has been synthesized and evaluated for anti-proliferative activity. 2-Alkene-1,3-indandione derivatives have been used as the precursors of a number of tricyclic compounds. The latter have been tested for anti-proliferative activity.

This is a preview of subscription content, log in to check access.

Scheme 1.
Scheme 2.
Scheme 3.
Fig. 1.


  1. 1

    Nugiel, D.A., Vidwans, A., Etzkorn, A.M., Rossi, K.A., Benfield, P.A., Burton, C. R., Cox, S., Doleniak, D., and Seitz, S.P., J. Med. Chem., 2002, vol. 45, p. 5224.

  2. 2

    Manpadi, M., Uglinskii, P.Y., Rastogi, S.K., Cotter, K.M., Wong, Y.S., Anderson, LA., Ortega, A.J., Van, S.S., Steelant, W.F., Rogelj, S., Tongwa, P., Antipin, M.Y., Magedov, I.V., and Komienko, A., Biomol. Chem., 2007, vol. 5, p. 3865.

  3. 3

    Ghorab, M.M. and Alsaid, M.S., Biomed. Res., 2015, vol. 26, p. 420.

  4. 4

    Tang, Z., Wu, C., Wang, T., Lao, K., Wang, Y., Liu, L., Muyaba, M., Xu, P., He, C., Luo, G., Qian, Z., Niu, S., Wang, L., Wang, Y., Xiao, H., You, Q., and Xiang, H., Eur. J. Med. Chem., 2016, vol. 118, p. 328.

    CAS  Article  PubMed  Google Scholar 

  5. 5

    Wang, Sh., Cao, L., Shi, H., Dong, Y., Sun, J., and Hu, Y., Chem. Pharm. Bull., 2005, vol. 53, p. 67.

  6. 6

    El-Rayyes, N.R., and Bahtiti, N.H., J. Heterocycl. Chem., 1989, vol. 26, p. 209.

    CAS  Article  Google Scholar 

  7. 7

    Samshuddina, S., Narayana, B., Sarojini, B.K., Yathirajan, H.S., and Raghavendra, R., Der Pharma Chemica, 2012, vol. 4, p. 1445.

    Google Scholar 

  8. 8

    Sharshira, E.M. and Hamada, N.M.M., Molecules, 2011, vol. 16, p. 7736.

    CAS  Article  PubMed  PubMed Central  Google Scholar 

  9. 9

    Goda, F.E., Abdel-Aziz, A.A.M., and Attef, O.A., Bioorg. Med. Chem., 2004, vol. 12, p. 1845.

  10. 10

    Chen, C., Lu, M., Liu, Z., Wan, J., Tu, Z., Zhang, T., and Yan, M., Open J. Med. Chem., 2013, vol. 3, p. 128.

    CAS  Article  Google Scholar 

  11. 11

    Amr, A.E., Abo-Ghalia, M.H., Moustafa, G., Al-Omar, M.A., Nossier, E.S., and Elsayed, E.A., Molecules, 2018, vol. 23, p. 2416,

    Article  PubMed Central  Google Scholar 

  12. 12

    Wurz, R.P., Pettus, L.H., Henkle, B., Sherman, L., Plant, M., Miner, K., McBride, H.J., Wong, L.M., Saris, C.J., Lee, M.R., Chmait, S., Mohr, C., Hsieh, F., and Tasker, A.S., Bioorg. Med. Chem. Lett., 2010, vol., 20, p. 1680.

  13. 13

    Chaikuad, A., Tacconi, E.; Zimmer, J., Liang, Y., Gray, N.S., Tarsounas, M., and Knapp, S.A., Nat. Chem. Biol., 2014, vol. 10, p. 853.

  14. 14

    Blake, J.F., Burkard, M., Chan, J., Chen, H., Chou, K.J., Diaz, D., Dudley, D.A., Gaudino, J.J., Gould, S.E., Grina, J., Hunsaker, T., Liu, L., Martinson, M., Moreno, D., Mueller, L., Orr, C., Pacheco, P., Qin, A., Rasor, K., Ren, L., Robarge, K., Shahidi-Latham, S., Stults, J., Sullivan, F., Wang, W., Yin, J., Zhou, A., Belvin, M., Merchant, M., Moffat, J., and Schwarz, J.B., J. Med. Chem., 2016, vol. 59, p. 5650.

    CAS  Article  PubMed  Google Scholar 

  15. 15

    Elzahabi, H.S.A., Nossier, E.S., Khalifa, N.M., Alasfoury, R.A., and El-Manawat, M.A., J. Enzy. Inh. Med. Chem., 2018, vol. 33, p. 546.

    CAS  Article  Google Scholar 

Download references


Authors are grateful to King Saud University for funding the work through Researchers Supporting Project (project no. RSP-2019/66).

Author information



Corresponding author

Correspondence to A. E. Amr.

Ethics declarations

No conflict of interest was declared by the authors.

Rights and permissions

Reprints and Permissions

About this article

Verify currency and authenticity via CrossMark

Cite this article

Abd-Elghaffar, H.S., El-Hashash, M.A., Mohamed, S.F. et al. Synthesis and Anti-Proliferative Activity of Novel Tricyclic Compounds Derived from 2-Substituted 1,3-Indandione. Russ J Gen Chem 90, 686–696 (2020).

Download citation


  • 1,3-indandione
  • anti-proliferative
  • p38αMAPK and ERK1/2 protein kinases
  • molecular modeling