Synthesis and anti-breast cancer activity of azole derivatives / 第二军医大学学报

ABSTRACT

Objective To design and synthesize a new series of efficient, low toxicity azole derivatives using antifungal drug ketoconazole as the lead compound and to explore their anti-breast cancer activity. Methods Based on the docking mode of ketoconazole with estrogen receptor. We designed and synthesized eleven derivatives, whose 2, 4-dichlorophenyl and triazole ring were retained and the side chains were modified. Then the in vitro anticancer activities against breast cancer cells MDA- MB-231 and MCF-7 were determined by MTT using tamoxifene as the positive control drug. Results and Conclusion The synthesized compounds have been reported for the first time and they have been confirmed by1HNMR and13CNMR. The synthesized azole derivatives have greater inhibitory effects than tamoxifene against breast cancer MDA MB-231 cells.