Nonsteroidal aromatase inhibitor 1 (Compound 13h) is a nonsteroidal aromatase (CYP19A1) inhibitor (IC50=0.09 nM). Nonsteroidal aromatase inhibitor 1 has potential for breast cancer research. Nonsteroidal aromatase inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Nonsteroidal aromatase inhibitor 1 (0.001 pM-100 pM; 1 h) treatment shows excellent aromatase inhibition activity[1].Nonsteroidal aromatase inhibitor 1 (1 μM; 48 h) treatment has no impact on MCF-10A or MDA-MB-231 growth[1].
References:
[1]. Ahmed G Eissa, et al. 4th generation nonsteroidal aromatase inhibitors: An iterative SAR-guided design, synthesis, and biological evaluation towards picomolar dual binding inhibitors. Eur J Med Chem. 2022 Jul 6;240:114569.