RH-1

RH-1 is a small molecule bioreductive anticancer agent designed to exploit the overexpression of NAD(P)H quinone oxidoreductase 1 (NQO1/DT-diaphorase) in many solid tumors. Upon two-electron reduction by NQO1, which is highly expressed in certain cancers such as lung, breast, and colorectal tumors, RH-1 becomes activated. This activation leads to the opening of aziridine rings within the molecule and results in DNA alkylation and cross-linking. The subsequent DNA damage induces apoptosis through both caspase-dependent and caspase-independent pathways involving mitochondrial disruption and nuclear translocation of apoptosis-inducing factors. Preclinical studies have shown potent anti-tumor activity both in vitro and in vivo. Clinical development has included phase I trials for advanced solid tumors and non-Hodgkin lymphoma[4][5][3][1].

Other names

2,5-diaziridinyl-3-hydroxymethyl-6-methyl-1,4-benzoquinoneRH1RH-1RH 1