Design, synthesis, molecular docking, and biological studies of novel phytoestrogen-tanaproget hybrids

作者：Kumar Sumit; Verma Nishant; Kumar Nikhil; Patel Alok; Roy Partha; Pruthi Vikas; Ahmed Naseem

来源：Synthetic Communications, 2016, 46(5): 460-474.

DOI：10.1080/00397911.2016.1144768

• Anticancer activity
• antimicrobial activity
• docking study
• estrogen and progesterone receptors
• phytoestrogen-tanaproget hybrids

A diverse range of novel and highly functionalized flavonoid-based tanaproget hybrids were synthesized and evaluated in vitro for their antimicrobial and antiproliferative activities. Novel products were synthesized in good yields (81-95%) under Pd-catalyzed reaction from bromo flavones and tanaproget boronic acids within 18-20min at 60 degrees C. Bioassay results exhibited excellent activities against both hormone-dependent and hormone-independent human breast cancer cells (MCF-7, MDA-MB-231, DU-145, PC-3, and HeLa). Among them, compounds 4e, 9a, 9c, 9e, 9g, 9h, 9m, and 9n displayed excellent activity. Compounds 4d, 4o, and 9o were found equally potent against C. albicans compared to fluconazole. Compound 5c showed better antibacterial activity against S. aureus. Compounds 5a, 9i, 9o, and 10c have shown admirable antibacterial activity against E. coli.

• 出版日期2016