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Novel D-modified heterocyclic androstane derivatives as potential anticancer agents: Synthesis, characterization, in vitro and in silico studies.
Sestic, Tijana Lj; Ajdukovic, Jovana J; Bekic, Sofija S; Celic, Andjelka S; Stojanovic, Sanja T; Najman, Stevo J; Marinovic, Maja A; Petri, Edward T; Skoric, Dusan D; Savic, Marina P.
Affiliation
  • Sestic TL; Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences, University of Novi Sad, Trg Dositeja Obradovica 3, 21000 Novi Sad, Serbia.
  • Ajdukovic JJ; Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences, University of Novi Sad, Trg Dositeja Obradovica 3, 21000 Novi Sad, Serbia. Electronic address: jovana.ajdukovic@dh.uns.ac.rs.
  • Bekic SS; Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences, University of Novi Sad, Trg Dositeja Obradovica 3, 21000 Novi Sad, Serbia.
  • Celic AS; Department of Biology and Ecology, Faculty of Sciences, University of Novi Sad, Trg Dositeja Obradovica 2, 21000 Novi Sad, Serbia.
  • Stojanovic ST; Department of Biology and Human Genetics, Faculty of Medicine, University of Nis, 18108 Nis, Serbia; Department for Cell and Tissue Engineering, Scientific Research Center for Biomedicine, Faculty of Medicine, University of Nis, 18108 Nis, Serbia.
  • Najman SJ; Department of Biology and Human Genetics, Faculty of Medicine, University of Nis, 18108 Nis, Serbia; Department for Cell and Tissue Engineering, Scientific Research Center for Biomedicine, Faculty of Medicine, University of Nis, 18108 Nis, Serbia.
  • Marinovic MA; Department of Biology and Ecology, Faculty of Sciences, University of Novi Sad, Trg Dositeja Obradovica 2, 21000 Novi Sad, Serbia.
  • Petri ET; Department of Biology and Ecology, Faculty of Sciences, University of Novi Sad, Trg Dositeja Obradovica 2, 21000 Novi Sad, Serbia.
  • Skoric DD; Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences, University of Novi Sad, Trg Dositeja Obradovica 3, 21000 Novi Sad, Serbia.
  • Savic MP; Department of Chemistry, Biochemistry and Environmental Protection, Faculty of Sciences, University of Novi Sad, Trg Dositeja Obradovica 3, 21000 Novi Sad, Serbia.
J Steroid Biochem Mol Biol ; 233: 106362, 2023 10.
Article in En | MEDLINE | ID: mdl-37451557
ABSTRACT
Cancer remains a major health concern worldwide. The most frequently diagnosed types of cancer are caused by abnormal production or action of steroid hormones. In the present study, the synthesis and structural characterization of new heterocyclic androstane derivatives with D-homo lactone, 17α-(pyridine-2''-ylmethyl) or 17(E)-(pyridine-2''-ylmethylidene) moiety are presented. All compounds were evaluated for their anti-proliferative activity against HeLa cervical cancer cell line and non-cancerous kidney MDCK cells, where A-homo lactam compound 9A showed the greatest selectivity. Based on in vitro binding assays, N-formyl lactam compound 18 appeared to be the strong and isoform-selective ligand for ERα, while compound 9A displayed binding affinity for the GR-LBD, but also inhibited aldo-keto reductase 1C4 enzyme. Out of four selected compounds, methylpyrazolo derivative 13 showed potential for aromatase binding, while in silico studies provided insight into experimentally confirmed protein-ligand interactions.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Androstanes / Antineoplastic Agents Limits: Humans Language: En Journal: J Steroid Biochem Mol Biol Journal subject: BIOLOGIA MOLECULAR / BIOQUIMICA Year: 2023 Document type: Article
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Androstanes / Antineoplastic Agents Limits: Humans Language: En Journal: J Steroid Biochem Mol Biol Journal subject: BIOLOGIA MOLECULAR / BIOQUIMICA Year: 2023 Document type: Article