Synthesis and antitumor activity of novel pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-5-one derivatives

Hala B El-Nassan

doi:10.1016/j.ejmech.2011.02.055

Synthesis and antitumor activity of novel pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-5-one derivatives

Eur J Med Chem. 2011 Jun;46(6):2031-6. doi: 10.1016/j.ejmech.2011.02.055. Epub 2011 Mar 3.

Author

Hala B El-Nassan¹

Affiliation

¹ Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 33 Kasr El-Aini Street, Cairo 11562, Egypt. [email protected]

PMID: 21429629
DOI: 10.1016/j.ejmech.2011.02.055

Abstract

A series of new pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidines with different substituents at position 3 were synthesized. The effect of the newly synthesized compounds was tested in vitro on human breast adenocarcinoma cell line (MCF7). Some of the synthesized compounds exploited potent antitumor activity, especially the 3-amino derivative 12 which displayed the highest activity among the test compounds with IC50 equal to 3.74 μg/mL.

MeSH terms

Antineoplastic Agents / chemical synthesis
Antineoplastic Agents / chemistry
Antineoplastic Agents / pharmacology*
Cell Line, Tumor
Cell Survival / drug effects
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Molecular Structure
Pyrimidinones / chemical synthesis
Pyrimidinones / chemistry
Pyrimidinones / pharmacology*
Stereoisomerism
Structure-Activity Relationship
Triazoles / chemical synthesis
Triazoles / chemistry
Triazoles / pharmacology*

Substances

3-amino-6-(4-chlorophenyl)-8-phenyl-1H-pyrido(2,3-d)(1,2,4)triazolo(4,3-a)pyrimidin-5-one
Antineoplastic Agents
Pyrimidinones
Triazoles