Chalcone-benzoxaborole hybrids as novel anticancer agents

Bioorg Med Chem Lett. 2016 Dec 1;26(23):5797-5801. doi: 10.1016/j.bmcl.2016.10.024.

Jiong Zhang ¹, Fei Yang ¹, Zhitao Qiao ¹, Mingyan Zhu ¹, Huchen Zhou ²

Affiliations

1 State Key Laboratory of Microbial Metabolism, School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China.
2 State Key Laboratory of Microbial Metabolism, School of Pharmacy, Shanghai Jiao Tong University, Shanghai, China; Chemical Biology Division of Shanghai Universities E-Institutes, Key Laboratory of Cell Differentiation and Apoptosis of Chinese Ministry of Education, Shanghai Jiao Tong University School of Medicine, Shanghai, China. Electronic address: hczhou@sjtu.edu.cn.

PMID: 28327308 DOI: 10.1016/j.bmcl.2016.10.024

Abstract

In this study, we report the synthesis of a series of chalcone-benzoxaborole hybrid molecules and the evaluation of their Anticancer activity. Their Anticancer potency and toxicity were tested on three human Cancer cell lines and two normal cell lines. The 4-fluoro compound 15 was found to be the most potent compound with an IC₅₀ value of 1.4μM on SKOV3 cells. The 4-iodo compound 18 and 3-methyloxy-4-amino compound 47 showed good potency on SKOV3 cells while exhibiting low toxicity on normal cells. This work extended the application of benzoxaboroles to the field of Anticancer research.

Keywords

Anticancer; Benzoxaborole; Drug discovery; Structure–activity relationship.

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