Phenylpyrrole-based HDAC inhibitors: Synthesis, molecular modeling and biological studies
| Autor: | Samuele Maramai, Manfred Jung, Sandra Gemma, Lucia Altucci, Ettore Novellino, Johanna Senger, Concetta Iside, Margherita Brindisi, Giuseppe Campiani, Alfonso Ciotta, Angela Nebbioso, Simone Brogi, Caterina Cavella, Stefania Lamponi, Stefania Butini |
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| Přispěvatelé: | Brindisi, Margherita, Cavella, Caterina, Brogi, Simone, Nebbioso, Angela, Senger, Johanna, Maramai, Samuele, Ciotta, Alfonso, Iside, Concetta, Butini, Stefania, Lamponi, Stefania, Novellino, Ettore, Altucci, Lucia, Jung, Manfred, Campiani, Giuseppe, Gemma, Sandra |
| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: |
Models
Molecular 0301 basic medicine Gene isoform drug design enzyme inhibitors Cell enzyme inhibitor Histone Deacetylase 1 antitumor agents bioinformatics epigenetics HDAC Histone Deacetylase 6 Histone Deacetylases 03 medical and health sciences Histone H3 Drug Discovery medicine Humans Pyrroles Pharmacology bioinformatic Molecular Structure biology HDAC6 HDAC1 In vitro Histone Deacetylase Inhibitors 030104 developmental biology medicine.anatomical_structure Histone Biochemistry Acetylation antitumor agent biology.protein Molecular Medicine |
| Zdroj: | Future medicinal chemistry 8 (2016): 1573–1587. doi:10.4155/fmc-2016-0068 info:cnr-pdr/source/autori:Brindisi, Margherita; Cavella, Caterina; Brogi, Simone; Nebbioso, Angela; Senger, Johanna; Maramai, Samuele; Ciotta, Alfonso; Iside, Concetta; Butini, Stefania; Lamponi, Stefania; Novellino, Ettore; Altucci, Lucia; Jung, Manfred; Campiani, Giuseppe; Gemma, Sandra/titolo:Phenylpyrrole-based HDAC inhibitors: synthesis, molecular modeling and biological studies/doi:10.4155%2Ffmc-2016-0068/rivista:Future medicinal chemistry (Print)/anno:2016/pagina_da:1573/pagina_a:1587/intervallo_pagine:1573–1587/volume:8 |
| DOI: | 10.4155/fmc-2016-0068 |
| Popis: | Aim: Histone deacetylases (HDACs) regulate the expression and activity of numerous proteins involved in the initiation and progression of cancer. Currently, three hydroxamate-containing HDAC pan-inhibitors have been approved as antitumor agents. Results: We herein present the development of a series of novel phenylpyrrole-based derivatives stemmed from combined computational and medicinal chemistry efforts to rationally modulate HDAC1/6 isoform selectivity. In vitro activity on HDAC1 and HDAC6 isoforms and the effects of selected analogs on histone H3 and α-tubulin acetylation levels were determined. Cell-based data evidenced, for selected compounds, a promising antitumor potential and low toxicity on normal cells. Conclusion: The newly developed compounds represent a valuable starting point for the development of novel anticancer agents. |
| Databáze: | OpenAIRE |
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