Anti-tumor application of a small molecular organic compound fn-01
A compound and application technology, applied in the field of medicinal chemistry, can solve problems such as unclear mechanism of action, few structure types, and low inhibition efficiency
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[0015] Antitumor activity test of compound (I) (FN-01)
[0016] Compound FN-01 of the present invention has been carried out IDO1 inhibitory experiment, following is the pharmacological test and result of compound of the present invention:
[0017] IDO enzyme can catalyze the pyrrole epoxidation cleavage on tryptophan to produce N'-formylkynurenine. At room temperature, mix 40nM IDO enzyme and 900uM L-tryptophan, and add reaction buffer (20mM ascorbate, 3.5uM methylene blue and 0.2mg / mL catalase in 50mM potassium phosphate bufferpH 6.5), at room temperature React for three hours, then perform UV measurement on a microplate reader, the detection wavelength is 321nm. The instrument reading conversion is: % activity = [(A-Ab) / (At-Ab)] × 100, and then use Prism GraphPad sofeware software Fit calculation IC 50 value.
[0018] The test results are shown in Table 1:
[0019] Table 1. FN-01 inhibition test on IDO1
[0020] sample number
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