These phosphorus dendron-based micelles showed moderate to high (IC50 = 0.2–50 μM) anti-proliferative activities themselves against a panel of tumor cell lines, including lung carcinoma A549, breast carcinoma MCF7, breast carcinoma metastasis MDA-MB-231, prostate carcinoma PC3, brain glioblastoma U87-MG, acute promyelocytic leukemia HL60, chronic myelogenous leukemia K562, myelogenous leukemia K562R (doxorubicin resistant due to high P-glycoprotein expression) and colorectal carcinoma HCT116. This evidence concerns the gene ABCB1 and neoplasm.