MedChemComm · 2010 · 24 citations · 19 references
Molecular PharmacologyMedicinal ChemistryMolecular ModelingChemoprevention StrategyPotent Anticancer AgentsMedicineIndoline-1-benzenesulfonamide 15Tubulin PolymerizationNovel ClassBiological EvaluationAnti-cancer AgentDrug DevelopmentCompound 15PharmacologyRadiation OncologyPharmaceutical ChemistryDrug Discovery
A series of 7-arylindoline-1-benzenesulfonamides were prepared and evaluated for anticancer activity. 7-(4′-Cyanophenyl)indoline-1-benzenesulfonamide 15 exhibited substantial antiproliferative activity with IC50 values ranging from 17–32 nM against a variety of human cancer cell lines, including MDR resistant line. Compound 15 (IC50 = 1.5 μM) also showed more potent inhibition of tubulin polymerization than 4a (combretastatin A-4, IC50 = 2.0 μM) and displayed strong binding to the colchicine binding site of the tubulin.
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Combretastatin A-4, an agent that displays potent and selective toxicity toward tumor vasculature.
G. Dark, S A Hill, Vivien E. Prise et al. · PubMed · 1997 · 624 citations
Differentiation and Definition of Vascular-Targeted Therapies
Dietmar W. Siemann, Michael C. Bibby, G. Dark et al. · Clinical Cancer Research · 2005 · 267 citations · Full text