3-arylisoquinolinamine derivative

3-arylisoquinolinamine derivative is a 3-arylisoquinolinamine derivative with antitumor activity. IC50 & Target: IC50: 21 nM (breast MDA-MB-231), 19 nM (pancreas PANC-1), 17 nM (colon HCT 116), 19 nM (prostate PC3), 14 nM (ovary OVCAR-3), 32 nM (melanoma SK-MEL-28), 22 nM (kidney Caki-1), 32 nM (glioblastoma SNB19)^[1] In Vitro: 3-arylisoquinolinamine derivative is a 3-arylisoquinolinamine derivative, extracted from the reference[1], compound 7b.3-arylisoquinolinamine derivative (7b) shows more effective activity against Paclitaxel-resistant HCT-15 human colorectal cancer cell lines when compared to the original cytotoxic cancer drug, Paclitaxel. The cell cycle dynamics is analyzed by flow cytometry. Treatment of human HCT-15 cells with 3-arylisoquinolinamine derivative (7b) blocks or delays the progression of cells from G0/G1 phase into S phase, and induces cell death. Treatment with 3-arylisoquinolinamine derivative (7b) also significantly inhibits the growth of tumors and enhances tumor regression in a Paclitaxel-resistant HCT-15 xenograft model. 3-arylisoquinolinamine derivative (7b) inhibits the cell growth at IC₅₀ value ranges from 14 nM to 32 nM in the human cancer cells tested. In cell cycle analysis using HCT-15 cells, treatment of 1 nM of 3-arylisoquinolinamine derivative (7b) displays a significant increase in G0/G1 phase at 24 h with a decrease in G2/M phase, but the increase of G0/G1 phase at 48 h is not significant. At higher concentration of 3-arylisoquinolinamine derivative (7b) (10 nM), there are a significant increase in G0/G1 phase and decrease in G2/M phase, and an emergence of sub-G1phase, at both 24 h and 48 h. 3-arylisoquinolinamine derivative (7b) blocks or delays the progression of cells from G0/G1 phase into S phase, and induces cell death^[1]. 3-arylisoquinolinamine derivative is a 3-arylisoquinolinamine derivative, extracted from the reference[1], compound 13. 3-arylisoquinolinamine derivative (compound 13) is tested in colon cancer cells and its antitumor activity is compared with Paclitaxel. 3-arylisoquinolinamine derivative (IC₅₀: 15 nM in HCT-15 cells, 17 nM in HCT116 cells) shows potent antiproliferative activities with IC₅₀ value in the low nanomolar range in both cells and higher antitumor activities than that of Paclitaxel against Paclitaxel-resistant HCT-15 colorectal cancer cells^[2]. In Vivo: 3-arylisoquinolinamine derivative (Compound 13) has higher antitumor efficacy (69.2 % inhibition) than that of the control drug, Paclitaxel (48.8 % inhibition) in the inhibition of growth of tumor in an animal model^[2].