Work

Novel Flavonoids with Antiproliferative Activities against Breast Cancer Cells

Year: 2011

Type: article

Abstract: A series of flavone analogues were synthesized and evaluated for their antiproliferation activity against breast cancer cells. The IC(50) of compound 10 and 24 were determined to be at 5 μM. These compounds were used as baits to screen breast cancer cDNA expression phage display proteome library. DNA sequencing of the binding phages suggests that eEF1A1 is a target protein for 10 and 24. Further optimization of these compounds led to the discovery of 39 with higher cytotoxic potency (IC(50) = 1 μM) and binding to eEF1A2. Biological and biochemical data suggest that eEF1A2 might be a therapeutic target and that 39 is an excellent lead compound for further development.

Source: Journal of Medicinal Chemistry

DOI: 10.1021/jm101440r

Authors: Nianhuan Yao, Chao-Yu Chen, Chun-Yi Wu, Kiyomi Motonishi, Hsing-Jien Kung, Kit S. Lam

Institutions: University of California Davis Medical Center, UC Davis Comprehensive Cancer Center, University of California, Davis

Language: English

Topic: Synthesis of Organic Compounds

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

SDG: Good health and well-being

Open Access status: green

Funder: National Cancer Institute