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Pomezia, Italy

Bigioni M.,Menarini Ricerche Pomezia | Ettorre A.,Menarini Ricerche Pomezia | Felicetti P.,Menarini Ricerche Pomezia | Mauro S.,Menarini Ricerche Pomezia | And 6 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

We report here the strategy used in our research group to find a new class of histone deacetylase (HDAC) inhibitors. A series of 5,11-dihydrodibenzo[b,e] azepine-6-ones alkylated on the amide nitrogen with an alkyl chain bearing an hydroxamic acids moiety at the end, has been designed (based upon the general motif for HDAC inhibitors), synthesized and tested. This allowed us to identify a new series of submicromolar HDAC inhibitors, which showed antiproliferative activity on HCT-116 colon carcinoma cells. © 2012 Elsevier Ltd. All rights reserved. Source


Rossi C.,Menarini Ricerche Pomezia | Porcelloni M.,Menarini Ricerche Pomezia | D'Andrea P.,Menarini Ricerche Pomezia | Fincham C.I.,Menarini Ricerche Pomezia | And 9 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

We report here the strategy used in our research group to find a new class of histone deacetylase (HDAC) inhibitors. A series of N-substituted 4-alkylpiperazine and 4-alkylpiperidine hydroxamic acids, corresponding to the basic structure of HDAC inhibitors (zinc binding moiety-linker-capping group) has been designed, prepared, and tested for HDAC inhibition. Linker length and aromatic capping group connection were systematically varied to find the optimal geometric parameters. A new series of submicromolar inhibitors was thus identified, which showed antiproliferative activity on HCT-116 colon carcinoma cells. © 2011 Elsevier Ltd. All rights reserved. Source


Rossi C.,Menarini Ricerche Pomezia | Fincham C.I.,Menarini Ricerche Pomezia | D'Andrea P.,Menarini Ricerche Pomezia | Porcelloni M.,Menarini Ricerche Pomezia | And 8 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

A series of N-substituted 4-alkylpiperidine hydroxamic acids, corresponding to the basic structure of histone deacetylase (HDAC) inhibitors (zinc binding moiety-linker-capping group) has been previously reported by our group. Linker length and aromatic capping group connection were systematically varied to find the optimal geometric parameters. A new series of submicromolar inhibitors was thus identified, which showed antiproliferative activity on HCT-116 colon carcinoma cells. We report here the second part of the strategy used in our research group to find a new class of HDAC inhibitors, namely the SAR study for the compounds bearing a sulfonyl group on the piperidine nitrogen. In the present work, we have considered both sulfonamides and sulfonyl ureas. © 2011 Elsevier Ltd. All rights reserved. Source


Animati F.,Menarini Ricerche Pomezia | Berettoni M.,Menarini Ricerche Pomezia | Bigioni M.,Menarini Ricerche Pomezia | Binaschi M.,Menarini Ricerche Pomezia | And 4 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

Glycosylated indolocarbazoles related to the antibiotic rebeccamycin represent an important class of antitumour drugs. In the course of our structure-activity relationship studies, new rebeccamycin analogues modified at the imide moiety were synthesised. The antiproliferative activity of the compounds was evaluated on three human cancer cell lines, A2780 (ovarian cancer), H460 (lung cancer), and GLC4 (small-cell lung cancer). The in vitro cytotoxicity of compounds 2 and 4, characterised respectively by a 1,3-dioxolan and (1,3-dioxolan-4-yl)methylene groups linked to the imide moiety, was higher than the reference compound, edotecarin. The effect of compound 2 in inducing tumour regression in the A2780 xenograft model was also investigated. © 2012 Elsevier Ltd. All rights reserved. Source

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