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Synthesis and antiproliferative activity of two new tiazofurin analogues with 2'-amido functionalities
Authors:Popsavin Mirjana  Torović Ljilja  Svircev Milos  Kojić Vesna  Bogdanović Gordana  Popsavin Velimir
Affiliation:1. Department of Chemistry, Faculty of Sciences, University of Novi Sad, Trg D. Obradovića 3, 21000 Novi Sad, Serbia and Montenegro;2. Institute of Oncology Sremska Kamenica, Institutski put 4, 21204 Sremska Kamenica, Serbia and Montenegro;1. Department of Chemistry, Faculty of Science, Karabuk University, 78050, Karabuk, Turkey;2. Department of Medical Microbiology, Faculty of Medicine, Giresun University, Giresun, 28100, Turkey;3. Department of Chemical Engineering, Faculty of Engineering and Architecture, Ahi Evran University, 40100, Kırşehir, Turkey;1. Laboratory of Molecular Signature Analysis, Division of Health Sciences, Osaka University Graduate School of Medicine, 1-7 Yamadaoka, Suita, Osaka 565-0871, Japan;2. Laboratory Chemicals Division, Wako Pure Chemical Industries, Ltd., 3-1-2 Doshomachi, Chuo-ku, Osaka, Osaka 540-8605, Japan;3. Department of Chemistry and Biochemistry, Texas Tech University, Lubbock, TX 79409-1061, USA;4. Department of Ophthalmology and Visual Sciences, Texas Tech University Health Sciences Center, Lubbock, TX 79430, USA;1. School of Science, Xi’an Jiaotong University, Xi’an 710049, China;2. School of Chemistry and Molecular Engineering, East China University of Science & Technology, Shanghai 200237, China;3. Department of Physics, Xinjiang University, Urumqi 830046, China;1. Fundação Oswaldo Cruz, Centro de Pesquisa Aggeu Magalhães, Laboratório de Imunogenética, CEP 50670-420, Recife, PE, Brazil;2. Universidade Federal de Pernambuco, Departamento de Ciências Farmacêuticas, CEP 50740-520, Recife, PE, Brazil;3. Fundação Oswaldo Cruz, Centro de Pesquisas Gonçalo Moniz, CEP 40296-710, Salvador, BA, Brazil;1. Chemistry Department, Faculty of Science, Suez Canal University, Ismailia, Egypt;2. Medicinal Chemistry Department, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt;3. Chemistry Department, Faculty of Science, Alexandria University, Alexandria, Egypt;4. Institute of Analytical Chemistry, Chemo and Biosensors, Universitätsstrasse 31, 93053 Regensburg, Germany
Abstract:Two novel tiazofurin analogues 2 and 3 were synthesized starting from d-glucose. The key step of the synthesis was the efficient one-step hydrogen sulfide-mediated conversion of 2-azido-3-O-acyl-ribofuranosyl cyanides to the corresponding 2-amido thiocarboxamides. Compounds 2 and 3 were evaluated for their in vitro antiproliferative activity against certain human tumour cell lines. Remarkably, compound 2 was found to be 570-fold more potent than tiazofurin against MCF-7 cells, while compound 3 showed the most powerful cytotoxicity against HT-29 cancer cells, being almost 100-fold more active than tiazofurin.
Keywords:
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