anthracenymethyl homospermidine

**Anthracenymethyl homospermidine** is a synthetic small molecule consisting of a homospermidine (4,4-triamine) backbone conjugated at the N(1)-position with a 9-anthracenylmethyl group. It acts as a selective substrate and inhibitor for the polyamine transporter (PAT), efficiently entering cells with active polyamine transport, including cancerous cells such as L1210 murine leukemia and A375 melanoma[2][3]. In biological evaluations, anthracenylmethyl homospermidine displays high affinity for the polyamine transporter, with reported Ki values in the low micromolar range, particularly in polyamine-depleted or transport-active cell models[3]. It induces cytotoxicity in cell lines with active polyamine transport, and microscopy studies reveal rapid formation of intracellular vesicles in melanoma cells after treatment[2][3]. Its primary mechanism appears to be competitive inhibition of polyamine uptake, disrupting polyamine homeostasis and inhibiting cell proliferation[2][3]. Anthracenylmethyl homospermidine has been used as a toxic probe in polyamine-transport inhibition assays and is considered a lead molecule for future polyamine blocking therapies, particularly in combination with biosynthesis inhibitors like DFMO[5].

Other names

anthracenylmethyl homospermidineN(1)-(anthracen-9-ylmethyl)homospermidine9-anthracenylmethyl-homospermidine