furamidine

Furamidine is also a selective and cell-permeable protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine (DB75) is abisbenzamidine derivative and an antiparasite agent. Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA.

Furamidine dihydrochloride (DB75 dihydrochloride) is a cell-permeable, selective small molecule inhibitor of protein arginine methyltransferase 1 (PRMT1) that also binds preferentially to strings of AT base pair sequences within the minor groove of DNA; it targets the PRMT1 enzyme active site primarily through a competitive mechanism with the protein substrate and is noncompetitive toward the cofactor, ultimately leading to the blockade of cell proliferation in various leukemia cell lines irrespective of their genetic lesions.

Pafuramidine (DB289) is an experimental prodrug of the orally active metabolite DB75, a potent antiparasitic compound with anti-malarial activity used in the study of parasitic infections and sleeping sickness.

Pafuramidine is an orally bioavailable prodrug of formamidine which was developed for the treatment of human African trypanosomiasis.

DB722 is a furamidine analogues with DNA binding activity. DB722 shows antiproliferative activity.