Synthesis and antiproliferative activity of some steroidal thiosemicarbazones,semicarbazones and hydrozones |
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| Institution: | 1. College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001, China;2. School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China;3. New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, China;1. Department of Organic Chemistry, University of Szeged, Dóm tér 8, H-6720 Szeged, Hungary;2. Department of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary;1. Steroid Research Laboratory, Department of Chemistry, Aligarh Muslim University, Aligarh 202 002, India;2. Interdisciplinary Unit of Biotechnology, Aligarh Muslim University, Aligarh 202 002, India;3. Department of Civil Engineering, Islamic University of Science and Technology, Kashmir 192122, India;1. College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou 450001, China;2. School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China;3. New Drug Research & Development Center, Zhengzhou University, Zhengzhou 450001, China;1. Department of Chemistry, Islamia College of Science and Commerce, Srinagar 190009, India;2. Department of Chemistry and Biochemistry, University of Arizona, Tucson 85721, USA;3. Department of Chemistry, University of Kashmir, Hazratbal, Srinagar 190002, India;1. Biochemistry and Molecular Biology Research Platform, College of Life Science, Northwest A&F University, Yangling, Shaanxi 712100, China;2. Shaanxi Engineering Center of Bio-resource Chemistry & Sustainable Utilization, College of Science, Northwest A&F University, Yangling, Shaanxi 712100, China |
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| Abstract: | Steroidal thiosemicarbazones, semicarbazones and hydrazones have received extensive attention of scientists recently because they exhibit some biological activities such as antibacterial, antiviral and anticancer. Using different steroids as starting materials, through different chemical methods, 24 steroidal compounds with thiosemicarbazone, semicarbazone or hydrazone groups in their structures, were synthesized, characterized by IR, NMR and MS. The antiproliferative activity of the compounds was evaluated against human gastric cancer (SGC-7901) and human liver cancer (Bel-7404) cells. The structure–activity relationship of these compounds was discussed. The results showed that compound 3 and 12a–12c exhibited significant inhibitory activity to Bel-7404 cells, and IC50 values of them were 4.2, 11.0, 7.4 and 15.0 μM respectively (Cisplatin, IC50: 11.6 μM). |
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| Keywords: | Cholesterol Stigmasterol Steroidal thiosemicarbazones Steroidal semicarbazones Antiproliferative activity |
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