Rhee, Hee-Kyung published the artcileSynthesis, cytotoxicity, and DNA topoisomerase II inhibitory activity of benzofuroquinolinediones, Application In Synthesis of 4584-49-0, the publication is Bioorganic & Medicinal Chemistry (2007), 15(4), 1651-1658, database is CAplus and MEDLINE.
Benzofuroquinolinediones (7c and 7d) were synthesized by base-catalyzed condensation of dichloroquinolinediones with phenolic derivatives Their dialkylaminoalkoxy derivatives (8i-8p) were prepared by reaction with various dialkylaminoalkyl chlorides. The cytotoxicity of the synthesized compounds was evaluated against eight types of human cancer cell lines, and their topoisomerase II inhibition was assessed. In general, the cytotoxicity of benzofuroquinolinediones (8i-8p) was similar or superior to that of doxorubicin and showed more potent inhibitory activity than naphthofurandiones (8a-8h). Also, most of the compounds exhibited excellent topoisomerase II inhibitory activity at a concentration of 5 μM and two compounds, 8d and 8i, showed IC50 values of 1.19 and 0.68 μM, resp., and were much more potent than etoposide (IC50 = 78.4 μM), but similar to doxorubicin (IC50 = 2.67 μM). However their inhibitory activity on topoisomerase I was lower, and 8d and 8i showed IC50 values of 42.0 and 64.3 μM, resp.
Bioorganic & Medicinal Chemistry published new progress about 4584-49-0. 4584-49-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Salt,Amine,Aliphatic hydrocarbon chain, name is 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride, and the molecular formula is C5H13Cl2N, Application In Synthesis of 4584-49-0.
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