2-ethylphenyl-4-(3-ethylureido)benzenesulfonate and fosbretabulin

2-ethylphenyl-4-(3-ethylureido)benzenesulfonate has been researched along with fosbretabulin* in 1 studies

Other Studies

1 other study(ies) available for 2-ethylphenyl-4-(3-ethylureido)benzenesulfonate and fosbretabulin

ArticleYear
Synthesis, biological evaluation, and structure-activity relationships of novel substituted N-phenyl ureidobenzenesulfonate derivatives blocking cell cycle progression in S-phase and inducing DNA double-strand breaks.
    Journal of medicinal chemistry, 2012, Jul-12, Volume: 55, Issue:13

    Twenty-eight new substituted N-phenyl ureidobenzenesulfonate (PUB-SO) and 18 N-phenylureidobenzenesulfonamide (PUB-SA) derivatives were prepared. Several PUB-SOs exhibited antiproliferative activity at the micromolar level against the HT-29, M21, and MCF-7 cell lines and blocked cell cycle progression in S-phase similarly to cisplatin. In addition, PUB-SOs induced histone H2AX (γH2AX) phosphorylation, indicating that these molecules induce DNA double-strand breaks. In contrast, PUB-SAs were less active than PUB-SOs and did not block cell cycle progression in S-phase. Finally, PUB-SOs 4 and 46 exhibited potent antitumor activity in HT-1080 fibrosarcoma cells grafted onto chick chorioallantoic membranes, which was similar to cisplatin and combretastatin A-4 and without significant toxicity toward chick embryos. These new compounds are members of a promising new class of anticancer agents.

    Topics: Animals; Anticarcinogenic Agents; Benzenesulfonates; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Chick Embryo; Chorioallantoic Membrane; Cisplatin; DNA Breaks, Double-Stranded; Histones; HT29 Cells; Humans; Imidazolidines; Jurkat Cells; Neoplasms; Phenylurea Compounds; Phosphorylation; S Phase; Stilbenes; Structure-Activity Relationship

2012
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