Synthesis and evaluation of antitumor activity of 5-[2-(3,5- diaryl-4,5-dihydro-pyrazol-1-yl)-2-oxo-ethylidene]-2,4-thiazolidinediones

  • D.Ya. Havrylyuk -
  • R.B. Lesyk -
Keywords: synthesis, 2,4-thiazolidinediones, acylation, antitumor activity

Abstract

Following reaction of 3,5-diaryl-4,5-dihydro-lH-pyrazoles and (2,4-thiazolidinedione-5-ylidene)-acetyl chloride 5-[2-(3,5-diaryl-4,5-dihydro-pyruzol-1-yl)-2-oxoethylidene]-2,4-thiazolidinediones were synthesized. Structure of synthesized compounds was confirmed by 1H spectra. Antitumor activity screening allowed us to identify «hit-compound» for next optimization of potential anticancer agents’ structure.

References

Gavriluk D.Ya. Synthesis, transformation, and biological activity of novel spiral and non-fused bicyclic derivatives based on 4-thiazolidone: Abstract. diss. ... Cand. formats. of sciences. - Lviv, 2007 -20s.

Gavriluk D.Y., Lesik RB, Matiychuk VS, Obushak MD // Jury, Organ. and the format. chemistry. - 2006. - Vol.4, no. 1 (13). -WITH. 42-47.

Zimenkovsky BS, Lesik RB 4-Thiazolidone. Chemistry, physiological action, prospects. - Vinnitsa: The New Book, 2004. - 106 p.

Zimenkovsky BS, Gavrilyuk D.Y., Lesik RB etc. // Pharmacist. . —2006. - № 6. - P. 41 - 48.

Lesik RB, Zimenkovsky BS, Golota SM, Lebiak MM // Ibid. - 2001. - № 5. - P. 57-63.

Lesik RB Synthesis and biological activity of condensed and non-condensed 4-azolidone heterocyclic systems: Abstract. diss .... Dr. Pharmacist. of sciences. - Lviv, 2004. - 40 p.

Alley M.C., Scudiero D.A., Monks P.A. et al. / / Cancer Research. - 1988 - Vol. 48. P. 589-601.

Carter R.H., Scherle P.A., MuckelbauerJ.A. et al. // Proc. Natl. Acad. Sci. U.S.A. - 2001. - Vol. 98 - P. 11879-11886.

Havrylyuk Dmytro, Zimenkovsky Botys, Vasylenko Olexandr et al. / / European J. of Medicinal Chemistry. - 2008. - Vol. 44. P. 1396-1404, doi: 10.1016 / j.ejmech.2008.09.032.

Erhan Palaskaa, Mutlu Aytemira, l. Tayfun Uzbuyb et al. // Eur. J. Med. Chem. - 2001. - Vol. 36. P. 539-543.

Grever M R., Schepartz S.A., Chabner B.A. / / Seminars in Oncology. - 1992 - Vol. 19, No. 6. - P.622-638.

Published
2009-06-25
How to Cite
Havrylyuk, D., & Lesyk, R. (2009). Synthesis and evaluation of antitumor activity of 5-[2-(3,5- diaryl-4,5-dihydro-pyrazol-1-yl)-2-oxo-ethylidene]-2,4-thiazolidinediones. Farmatsevtychnyi Zhurnal, (3), 51-55. Retrieved from https://pharmj.org.ua/index.php/journal/article/view/981
Section
Original Articles

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