Synthesis and antitumor activity of novel 6-aryl and 6-alkylpyrazolo[3,4-d]pyrimidin-4-one derivatives

Mervat M el-Enany; Mona M Kamel; Omneya M Khalil; Hala B el-Nassan

doi:10.1016/j.ejmech.2010.08.048

Synthesis and antitumor activity of novel 6-aryl and 6-alkylpyrazolo[3,4-d]pyrimidin-4-one derivatives

Eur J Med Chem. 2010 Nov;45(11):5286-91. doi: 10.1016/j.ejmech.2010.08.048. Epub 2010 Sep 16.

Authors

Mervat M el-Enany¹, Mona M Kamel, Omneya M Khalil, Hala B el-Nassan

Affiliation

¹ Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Kasr El-Aini street, Cairo 11562, Egypt.

PMID: 20846758
DOI: 10.1016/j.ejmech.2010.08.048

Abstract

A series of new 6-arylpyrazolo[3,4-d]pyrimidin-4-ones and 6-alkylpyrazolo[3,4-d]pyrimidin-4-ones were synthesized. Some of the newly synthesized compounds were tested in vitro on human colon tumor cell line (HCT116). Most of the test compounds exploited potent antitumor activity, especially compound 10a which displayed the highest activity among the test compounds with IC(50) equal to 0.47 μg/mL.

MeSH terms

Antineoplastic Agents / chemical synthesis*
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Drug Screening Assays, Antitumor
Humans
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy
Pyrimidinones / chemical synthesis*
Pyrimidinones / pharmacology*
Spectrophotometry, Infrared

Substances

Antineoplastic Agents
Pyrimidinones