biostudies-literatureNguyen HPMinistry of EducationBộ Giáo dục và Ðào tạoMinistry of Science and ICT, South Korea22108-22118https://www.ebi.ac.uk/biostudies/studies/S-EPMC9364358biostudies-literatureUnknown12(34)Multiple myeloma is a deadly cancer that is a complex and multifactorial disease. In the present study, 12 belinostat derivatives (four resynthesized and eight new), HDAC inhibitors, were resynthesized <i>via</i> either Knoevenagel condensation, or Wittig reaction, or Heck reaction. Then an evaluation of the antiproliferative activities against myeloma cells MOPC-315 was carried out. Amongst them, compound 7f was the most bioactive compound with an IC₅₀ of 0.090 ± 0.016 μM, being 3.5-fold more potent than the reference belinostat (IC₅₀ = 0.318 ± 0.049 μM). Furthermore, we also confirmed the inhibitory activity of 7f in a cellular model. Additionally, we found that the inhibitory activity of 7f against histone deacetylase 6 catalytic activity (HDAC6) is more potent thaRSC advancesAnti-multiple myeloma potential of resynthesized belinostat derivatives: an experimental study on cytotoxic activity, drug combination, and docking studies.PMC93643582018R1A6A1A03025523B2019-TCT-37 (TCT-05)2020R1A2B5B020023772019M3E5D1A02069623Nguyen CQTuan NTVan Ky NHoa TPNguyen HPLe Dang QHue BTBQuoc Chau Thanh NNhu Thao HPham MQDuy Binh TTran QYang SGfalseAnti-multiple myeloma potential of resynthesized belinostat derivatives: an experimental study on cytotoxic activity, drug combination, and docking studies.Multiple myeloma is a deadly cancer that is a complex and multifactorial disease. In the present study, 12 belinostat derivatives (four resynthesized and eight new), HDAC inhibitors, were resynthesized <i>via</i> either Knoevenagel condensation, or Wittig reaction, or Heck reaction. Then an evaluation of the antiproliferative activities against myeloma cells MOPC-315 was carried out. Amongst them, compound 7f was the most bioactive compound with an IC₅₀ of 0.090 ± 0.016 μM, being 3.5-fold more potent than the reference belinostat (IC₅₀ = 0.318 ± 0.049 μM). Furthermore, we also confirmed the inhibitory activity of 7f in a cellular model. Additionally, we found that the inhibitory activity of 7f against histone deacetylase 6 catalytic activity (HDAC6) is more potent tha2022-01-01T00:00:00Z2022 Aug2026-05-09T19:35:05.067Z2025-04-21T14:47:28.683ZS-EPMC93643583604310510.1039/d2ra01969h