Synthesis and Evaluation of Ethyl 2,4-dioxo-4-arylbutanoate Derivatives as Src Kinase Inhibitors

Akbarzadeh, T.; Rafinejad, A.; Fallah-Tafti, A.; Tiwari, R.; Nasrolahi Shirazi, A.; Mandal, D.; Parang, K.; Foroumadi, A.

Synthesis and Evaluation of Ethyl 2,4-dioxo-4-arylbutanoate Derivatives as Src Kinase Inhibitors

Document Type : Final File

Authors

T. Akbarzadeh ¹

A. Rafinejad ¹

A. Fallah-Tafti ¹

R. Tiwari ²

A. Nasrolahi Shirazi ²

D. Mandal ²

K. Parang ²

A. Foroumadi ³

¹ 1 Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Islamic Republic of Iran

² 2 Department of Biomedical and Pharmaceutical Sciences, College of Pharmacy, University of Rhode Island, Kingston, RI 02881, USA

³ 3 Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Research Center, Tehran University of Medical Sciences, Tehran, Islamic Republic of Iran

Abstract

In this work, different ethyl 2,4-dioxo-4-arylbutanoate derivatives were prepared and evaluated for their Src Kinase inhibitory activity. For this purpose, the appropriate substituted acetophenone derivatives reacted with diethyl oxalate in the presence of sodium ethoxide in dried ethanol to give the corresponding products. All compounds showed moderate activities comparing with staurosporine as the reference drug.

Keywords

Ethyl 2,4-dioxo-4-arylbutanoates

Src kinase

cancer