Development of Furo[2,3-b]quinoline Derivatives with Anti-Breast Cancer Property by Targeting Topoisomerase II

Title:Development of Furo[2,3-b]quinoline Derivatives with Anti-Breast Cancer Property by Targeting Topoisomerase II

Volume: 21 Issue: 12

Author(s): Ying Wang, Na Li, Neng Jiang, Li Chen*Jianbo Sun*

Affiliation:

• Department of Natural Medicinal Chemistry, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009,China

• Department of Natural Medicinal Chemistry, School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 210009,China

Keywords: Furo[2, 3-b]quinolone, breast cancer, design and synthesis, cytotoxic activity, topoisomerase II, MTT.

Abstract: A number of novel furo[2,3-b]quinoline derivatives were designed and synthesized by introducing different substituted anilines and phenols to C4-position of furo[2,3-b]quinoline. All target compounds were evaluated in vitro against two human breast cancer cell lines (MCF-7 and MDA-MB-231) and one normal breast cell (MCF-10A) by MTT (3-[4,5-dimethylthylthiazol-2-yl]-2,5 diphenyltetrazolium broide, Thiazolyl blue) method. Most derivatives showed significant cytotoxic activity on the two breast cancer cells with IC₅₀ values in the range of (5.60-26.24 μM) and a certain selectivity, especially in the inhibition of MDA-MB-231. More notably, they were less toxic to normal breast cell (MCF-7-10A). Compound I₇ could be considered as an ideal selective candidate for further study. Mechanism studies showed that I₇ could inhibit the proliferation of cells by arresting MDA-MB-231 cell cycle at G2/M phase. Overall, as a novel furo[2,3-b]quinoline derivative, I₇ exhibited an excellent inhibitory effect in MDA-MB-231 cell and was worthy of in-depth study.

Cite this article as:

Wang Ying , Li Na , Jiang Neng , Chen Li *, Sun Jianbo *, Development of Furo[2,3-b]quinoline Derivatives with Anti-Breast Cancer Property by Targeting Topoisomerase II, Anti-Cancer Agents in Medicinal Chemistry 2021; 21 (12) . https://dx.doi.org/10.2174/1871520620999201103201348