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2. Synthesis of novel pentacyclic [beta]-lactam antibacterial agents

Author

Andreotti, Daniele, Biondi, Stefano, Donati, Daniele, Lociuro, Sergio, and Pain, Gilles

Subjects
Antibacterial agents, Cyclic compounds -- Composition, Chemical research -- Analysis
Abstract

The search for new antibacterial agents still represents an active area of research. In this paper the synthesis of a new class of [beta]-lactam agents characterized by an interesting antibacterial profile is reported; together with a description of the most significant synthetic aspects encountered during this work. Key words: [beta]-lactams, pentacyclic, O-alkylation, trinem.

Published
2000

5. Cinnamic Anilides as New Mitochondrial Permeability Transition Pore Inhibitors Endowed with Ischemia-Reperfusion Injury Protective Effect in Vivo

Author

Fancelli, Daniele, primary, Abate, Agnese, additional, Amici, Raffaella, additional, Bernardi, Paolo, additional, Ballarini, Marco, additional, Cappa, Anna, additional, Carenzi, Giacomo, additional, Colombo, Andrea, additional, Contursi, Cristina, additional, Di Lisa, Fabio, additional, Dondio, Giulio, additional, Gagliardi, Stefania, additional, Milanesi, Eva, additional, Minucci, Saverio, additional, Pain, Gilles, additional, Pelicci, Pier Giuseppe, additional, Saccani, Alessandra, additional, Storto, Mariangela, additional, Thaler, Florian, additional, Varasi, Mario, additional, Villa, Manuela, additional, and Plyte, Simon, additional

Published
2014
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6. Reagent control in the aldol addition reaction of chiral boron enolates with chiral alpha-amino aldehydes. Total synthesis of (3S,4S)-statine

Author

Gennari, Cesare, Pain, Gilles, and Moresca, Daniela

Subjects
Aldehydes -- Reactivity, Chemical reactions -- Observations, Organoboron compounds -- Analysis, Biological sciences, Chemistry
Abstract

A aldol reaction between chiral N,N-dibenzylamino aldehyde and chiral boron enolate results in the formation of (3S,4S)-statine, a major component of pepstatine. Transition state computer modeling is used to prepare novel boron reagents which allow enantioselective preparation of ketone-derived anti and unsubstituted aldols. Undesirable diastereomers adulterate the aldol product, but these impurities can be eliminated by flash chromatography. The experimental procedure for the synthesis of (3S,4S)-statine is discussed.

Published
1995

7. Synthesis and Biological Evaluation of N-Hydroxyphenylacrylamides and N-Hydroxypyridin-2-ylacrylamides as Novel Histone Deacetylase Inhibitors

Author

Thaler, Florian, primary, Colombo, Andrea, additional, Mai, Antonello, additional, Amici, Raffaella, additional, Bigogno, Chiara, additional, Boggio, Roberto, additional, Cappa, Anna, additional, Carrara, Simone, additional, Cataudella, Tiziana, additional, Fusar, Fulvia, additional, Gianti, Eleonora, additional, di Ventimiglia, Samuele Joppolo, additional, Moroni, Maurizio, additional, Munari, Davide, additional, Pain, Gilles, additional, Regalia, Nickolas, additional, Sartori, Luca, additional, Vultaggio, Stefania, additional, Dondio, Giulio, additional, Gagliardi, Stefania, additional, Minucci, Saverio, additional, Mercurio, Ciro, additional, and Varasi, Mario, additional

Published
2009
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18. Synthesis of novel pentacyclic -lactam antibacterial agents

Author

Andreotti, Daniele, Biondi, Stefano, Donati, Daniele, Lociuro, Sergio, and Pain, Gilles

Abstract

The search for new antibacterial agents still represents an active area of research. In this paper the synthesis of a new class of -lactam agents characterized by an interesting antibacterial profile is reported; together with a description of the most significant synthetic aspects encountered during this work.Key words: -lactams, pentacyclic, O-alkylation, trinem.

Published
2000
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19. Synthesis of a simplified analogue of eleutherobin viaa Claisen rearrangement and ring closing metathesis strategyElectronic supplementary information (ESI) available: experimental procedure for the conversion of 5into 6and 9and spectroscopic data for 6and 7. See http://www.rsc.org/suppdata/cc/b4/b413426e/

Author

Chiang, Gary C. H., Bond, Andrew D., Ayscough, Andrew, Pain, Gilles, Ducki, Sylvie, and Holmes, Andrew B.

Abstract

The enantioselective synthesis of a simplified eleutherobin analogue 7by ring closing metathesis RCM of the 2,9-divinyl-substituted tetrahydro-oxonin 5is described; the analogue 7and an advanced intermediate 15revealed microtubule stabilising properties in the micromolar range.

Published
2005
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20. Synthesis and biological evaluation of N-hydroxyphenylacrylamides and N-hydroxypyridin-2-ylacrylamides as novel histone deacetylase inhibitors.

Author

Thaler F, Colombo A, Mai A, Amici R, Bigogno C, Boggio R, Cappa A, Carrara S, Cataudella T, Fusar F, Gianti E, di Ventimiglia SJ, Moroni M, Munari D, Pain G, Regalia N, Sartori L, Vultaggio S, Dondio G, Gagliardi S, Minucci S, Mercurio C, and Varasi M

Subjects
Acrylamides pharmacology, Antineoplastic Agents pharmacokinetics, Benzene Derivatives, Cell Proliferation drug effects, Colonic Neoplasms drug therapy, Drug Stability, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors pharmacokinetics, Enzyme Inhibitors therapeutic use, HeLa Cells, Histone Deacetylase Inhibitors pharmacokinetics, Histone Deacetylase Inhibitors therapeutic use, Humans, Pyridines, Structure-Activity Relationship, Xenograft Model Antitumor Assays, Acrylamides chemical synthesis, Antineoplastic Agents chemical synthesis, Histone Deacetylase Inhibitors chemical synthesis
Abstract

The histone deacetylases (HDACs) are able to regulate gene expression, and histone deacetylase inhibitors (HDACi) emerged as a new class of agents in the treatment of cancer as well as other human disorders such as neurodegenerative diseases. In the present investigation, we report on the synthesis and biological evaluation of compounds derived from the expansion of a HDAC inhibitor scaffold having N-hydroxy-3-phenyl-2-propenamide and N-hydroxy-3-(pyridin-2-yl)-2-propenamide as core structures and containing a phenyloxopropenyl moiety, either unsubstituted or substituted by a 4-methylpiperazin-1-yl or 4-methylpiperazin-1-ylmethyl group. The compounds were evaluated for their ability to inhibit nuclear HDACs, as well as for their in vitro antiproliferative activity. Moreover, their metabolic stability in microsomes and aqueous solubility were studied and selected compounds were further characterized by in vivo pharmacokinetic experiments. These compounds showed a remarkable stability in vivo, compared to hydroxamic acid HDAC inhibitors that have already entered clinical trials. The representative compound 30b showed in vivo antitumor activity in a human colon carcinoma xenograft model.

Published
2010
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