Synthesis and antiproliferative studies of 5-aryl-2-(3-thienylamino)-1,3,4-thiadiazoles |
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| Institution: | 1. Université de Lorraine, Laboratoire de Synthèse et Réactivité des Systèmes Moléculaires Complexes UMR-SRSMC 7565, Equipe Hécrin, 1 boulevard Arago, 57070 Metz Technopôle, France;2. Laboratoire de toxicologie, Université Libre de Bruxelles, Brussels, Belgium;1. Molecular Sciences and Candidate Optimization, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, United States;2. Neuroscience Discovery Biology, Research and Development, Bristol-Myers Squibb Company, 5 Research Parkway, Wallingford, CT 06492, United States;1. Ural Research Institute for Phthisiopulmonology, 22 Parts’ezda, 50, Ekaterinburg 620039, Russia;2. I. Postovsky Institute of Organic Synthesis, Ural Branch of the Russian Academy of Sciences, S. Kovalevskoy Str., 22, Ekaterinburg 620990, Russia;3. Ural Federal University, Mira St. 19, Ekaterinburg 620002, Russia;1. Chemistry Department, Faculty of Science, Al-Azhar University at Assiut, 71524 Assiut, Egypt;2. Chemistry Department, Faculty of Science (Girl''s), Al-Azhar University, Nasr City, Cairo, Egypt;3. Chemistry Department, Faculty of Science, Al-Azhar University, Nasr City, Cairo, Egypt;4. Photochemistry Department, National Research Center, El-Dokki, Giza, Egypt;1. Department of Physics, Ataturk University, 25240 Erzurum, Turkey;2. Ostim Vocational School, Gazi University, 06500 Ankara, Turkey;3. Department of Biology, Ataturk University, 25240 Erzurum, Turkey;4. Department of Physics, K.K. Education Faculty, Ataturk University, 25240 Erzurum, Turkey |
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| 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 μM on three cell lines. |
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| Keywords: | Thienylamino-1 3 4-thiadiazoles Thienylthiosemicarbazides Thienylisothiocyanates Antiproliferative agents MTT assay |
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