Design,synthesis, docking studies and biological evaluation of novel chalcone derivatives as potential histone deacetylase inhibitors |
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| Affiliation: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sohag University, 82524 Sohag, Egypt;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Al-Azhar University, 71524 Assiut, Egypt;3. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Al-Azhar University, 71524 Assiut, Egypt;4. Department of Biochemistry, Faculty of Pharmacy, Al-Azhar University, 71524 Assiut, Egypt;5. Department of Medicinal Chemistry, Faculty of Pharmacy, Assiut University, 71526 Assiut, Egypt;6. Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, 61519 Minia, Egypt;1. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, 11561, Cairo, Egypt;2. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA), Giza, Egypt;3. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy and Drug Manufacturing, Misr University for Science and Technology, Giza, Egypt;1. Institute of Oncology and Radiology of Serbia, Pasterova 14, 11000 Belgrade, Serbia;2. Faculty of Science, Department of Chemistry, University of Kragujevac, R. Domanovica 12, 34000 Kragujevac, Serbia;3. Laboratory for Radiobiology and Molecular Genetics, “Vinča” Institute of Nuclear Sciences, University of Belgrade, 11000 Belgrade, Serbia;4. Faculty of Pharmacy, Department of Organic Chemistry, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia;1. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut 71526, Assiut, Egypt;2. Pharmaceutical Chemistry Department, College of Pharmacy, Jouf University, Sakaka, Aljouf 2014, Saudi Arabia;3. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sohag University, 82524 Sohag, Egypt;4. Department of Chemistry, Faculty of Science, Sohag University, Sohag 82524, Egypt;5. Pharmacology Department, College of Pharmacy, Jouf University, Sakaka, Aljouf 2014, Saudi Arabia;6. Biochemistry Department, Faculty of Pharmacy, Nahda University, Beni-Suef, Egypt;1. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Al-Azhar University, 71524 Assiut, Egypt;2. Department of Medicinal Chemistry, Faculty of Pharmacy, Minia University, 61519 Minia, Egypt;3. Department of Pharmaceutical Chemistry, College of Pharmacy, Jouf University, Sakaka, Saudi Arabia |
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| Abstract: | A group of novel chalcone derivatives comprising hydroxamic acid or 2-aminobenzamide group as zinc binding groups (ZBG) were synthesized. The structure of the prepared compounds was fully characterized by IR, NMR and elemental microanalyses. Most of the tested compounds displayed strong to moderate HDAC inhibitory activity. Some of these compounds showed potent anti-proliferative activity against human HepG2, MCF-7 and HCT-116 cell lines. In particular, compounds 4a and 4b exhibited significant anti-proliferative activity against the three cell lines compared to SAHA as reference drug and displayed promising profile as anti-tumor candidates. The results indicated that these chalcone derivatives could serve as a promising lead compounds for further optimization as antitumor agents. |
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| Keywords: | Chalcone Histone deacetylase Docking Anti-proliferative HDAC inhibitors |
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