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BPTQ is a typical intercalator of DNA. It acts by inducing dose-dependent inhibitory effect on the proliferation of cancer cells by arresting cells at S and G2/M phase and activating the mitochondria-mediated apoptosis pathway.

BPTQ is a potent inhibitor against VEGFR1 and CHK2 with IC50 values of 0.54 and 1.70 μmol/L, respectively. BPTQ is also an intercalator of DNA with anticancer activities. BPTQ inhibits the proliferation of HL-60 cells by arresting cells at S and G2/M phase with an IC50 value of 12 μmol/L. BPTQ also activates the mitochondria-mediated Apoptosis pathway by a decrease in mitochondrial membrane potential, increase in the Bax:Bcl-2 ratio and activation of caspases[1][2].

[1] RohitKumar HG, et al. DNA intercalative 4-butylaminopyrimido[4',5':4,5]thieno(2,3-b)quinoline induces cell cycle arrest and apoptosis in leukemia cells. Cancer Chemother Pharmacol. 2015 Jun;75(6):1121-33. DOI:10.1007/s00280-015-2735-6
[2] Rohit Kumar H, et al. Inhibition of protein kinases by anticancer DNA intercalator, 4-butylaminopyrimido[4',5':4,5]thieno(2,3-b)quinoline. Acta Pharm Sin B. 2017 May;7(3):303-310. DOI:10.1016/j.apsb.2017.01.001