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Synthesis and antiproliferative studies of 5-aryl-2-(3-thienylamino)-1,3,4-thiadiazoles

Abstract : A series of 5-aryl-2-(3-thienylamino)-1,3,4-thiadiazoles 3a-m were synthesized in good yields in two steps starting from thiophen-3-isothiocyanates. Those compounds as well as the thiosemicarbazide intermediates 2a-m were screened for their antiproliferative activity against a panel of six cancer cell lines. Among them, two 5-aryl-2-(3-thienylamino)-1,3,4-thiadiazoles (3f and 3i) have shown very interesting results with IC50 < 10 mu M on three cell lines.
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Germain Revelant, Charlene Gadais, Veronique Mathieu, Gilbert Kirsch, Stéphanie Hesse. Synthesis and antiproliferative studies of 5-aryl-2-(3-thienylamino)-1,3,4-thiadiazoles. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2014, 24 (12), pp.2724-2727. ⟨10.1016/j.bmcl.2014.04.043⟩. ⟨hal-01494566⟩



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