Melatonin-Tamoxifen Conjugate

Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate made of Melatonin and Tamoxifen, serving as an effective antagonist of ER? (IC50 = 863 nM) . In cells expressing the hMT1 receptor, it binds to MLT receptors (Ki = 3.1 nM) and exhibits the ability to promote ?-arrestin activation (EC50 = 914 nM) and ERK activation (EC50 = 98 nM) . The IC50 values for Melatonin-Tamoxifen Conjugate in MCF-7, MDA-MB-231, and HT-1080 cell lines are 6.8 ?M, 6.4 ?M, and 1.7 ?M, respectively.