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CYP1B1 is mainly an extrahepatic enzyme which oxidatively metabolizes both endogenous (steroids; eicosanoids) and exogenous xenobiotics such aspolyaromatic hydrocarbons. TMS is a potent and selective inhibitor of CYP1B1, with an IC50 of 6 nM.1 It is 50-fold selective for the inhibition of CYP1B1 versus CYP1A1, making it a useful tool to differentiate between various CYP450 families.1 In cultured human colon cancer cells, TMS induces apoptosis and inhibits cell growth with an IC50 of 0.8 µg/ml.2
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1. Design, synthesis, and discovery of novel trans-
2. Resveratrol analog, 3,5,2',4'-