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Synthesis and biological activity of novel mycophenolic acid conjugates containing nitro-acridine/acridone derivatives.

Abstract：

:Hybrid pharmacophore anti-proliferative compounds, comprised of mycophenolic acid (MPA) and 1-nitroacridine/4-nitroacridone derivative have been synthesized and evaluated as inhibitors of five different leukemia cell lines (Jurkat, Molt-4, HL-60, CCRF-CEM, L1210) and human peripheral blood mononuclear cells from healthy donors. These conjugates possess different length of the linker between MPA and heterocyclic units. The type of heterocyclic part influenced their cytotoxic and anti-proliferative properties. Coupling of MPA 1 with 9-(ω-aminoalkyl)amino-1-nitroacridines 2 and 1-[(ω-aminoalkyl)-4-nitro-9(10H)]-acridones 3 was tested. Although all tested conjugates were active, compounds 4a-e exhibited the highest potency. Preliminary experiments with GMP suggested that the tested compounds acted as IMPDH inhibitors.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Malachowska-Ugarte M,Cholewinski G,Dzierzbicka K,Trzonkowski P

doi

10.1016/j.ejmech.2012.04.040

subject

Has Abstract

pub_date

2012-08-01 00:00:00

pages

197-201

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(12)00292-9

journal_volume

54

pub_type

杂志文章

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