Research Article Open Access

Anticancer Activities of Some New Synthesized Thiazolo[3,2-a]Pyrido[4,3-d]Pyrimidine Derivatives

Ashraf M. Mohamed1, Abdel-Galil E. Amr2, Musaed A. Alsharari1, Husam R.M. Al-Qalawi1, Mosa O. Germoush1 and Mohamed A. Al-Omar3
  • 1 Al-Jouf University, Saudi Arabia
  • 2 National Research Centre, Canada
  • 3 King Saud University, Saudi Arabia


Problem statement: This study describes the synthesis and anticancer activities of a new series of thiazolo[3,2-a]pyrimidines derivatives (2-7) using 3,5-bisarylmethylene-1-methyl-4- piperidone and 4-aryl-8-arylmethelene-6-methylpyrido[4,3-d]pyrimidine-2(1H)thiones as a starting materials. Approach: The antitumor activities of the newly synthesized compounds 4-7 were evaluated utilizing 60 different human tumor cell lines, representing leukemia, melanoma, lung, colon, brain, ovary, breast and prostate as well as kidney. Results: Some of the tested compounds exhibited better in vitro antitumor activities at low concentration (log10 GI50 = -4.7) against the used human tumor cell lines. Conclusion: From the obtained results, we can conclude that pyrimidine moieties fused to N-methylpipredine ring are essential for antitumor activities. In the present work, we can suggest that the anticancer activity is due to the presence of nitrogen heterocyclic rings and the presence of sulfur atom generally enhancing the activity.

American Journal of Biochemistry and Biotechnology
Volume 7 No. 2, 2011, 43-54


Submitted On: 30 May 2011 Published On: 23 August 2011

How to Cite: Mohamed, A. M., Amr, A. E., Alsharari, M. A., Al-Qalawi, H. R., Germoush, M. O. & Al-Omar, M. A. (2011). Anticancer Activities of Some New Synthesized Thiazolo[3,2-a]Pyrido[4,3-d]Pyrimidine Derivatives. American Journal of Biochemistry and Biotechnology, 7(2), 43-54.

  • 31 Citations



  • Synthesis
  • reactions
  • pyrimidinethione
  • thiazolopyrimidine
  • anticancer activity
  • starting materials
  • nitrogen heterocyclic
  • pyrimidines derivatives
  • biological activity