Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases

Ambra A. Grolla; Valeria Podestà; Maria Giovanna Chini; Simone Di Micco; Antonella Vallario; Armando A. Genazzani; Pier Luigi Canonico; Giuseppe Bifulco; Gian Cesare Tron; Giovanni Sorba; Tracey Pirali

doi:10.1021/jm801529c

Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases

Ambra A. Grolla, Valeria Podestà, Maria Giovanna Chini, Simone Di Micco, Antonella Vallario, Armando A. Genazzani, Pier Luigi Canonico, Giuseppe Bifulco, Gian Cesare Tron, Giovanni Sorba, Tracey Pirali

Dipartimento di Scienze del Farmaco

Risultato della ricerca: Contributo su rivista › Articolo in rivista › peer review

Abstract

HDAC inhibitors show great promise for the treatment of cancer. As part of a broader effort to explore the SAR of HDAC inhibitors, synthesis, biological evaluation, and molecular docking of novel Ugi products containing a zinc-chelating moiety are presented. One compound shows improved inhibitory potencies compared to SAHA, demonstrating that hindered lipophilic residues grafted on the peptide scaffold of the α-aminoacylamides can be favorable in the interaction with the enzyme.

Lingua originale	Inglese
pagine (da-a)	2776-2785
Numero di pagine	10
Rivista	Journal of Medicinal Chemistry
Volume	52
Numero di pubblicazione	9
DOI	https://doi.org/10.1021/jm801529c
Stato di pubblicazione	Pubblicato - 14 mag 2009

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Grolla, A. A., Podestà, V., Chini, M. G., Di Micco, S., Vallario, A., Genazzani, A. A., Canonico, P. L., Bifulco, G., Tron, G. C., Sorba, G., & Pirali, T. (2009). Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases. Journal of Medicinal Chemistry, 52(9), 2776-2785. https://doi.org/10.1021/jm801529c

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title = "Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases",

abstract = "HDAC inhibitors show great promise for the treatment of cancer. As part of a broader effort to explore the SAR of HDAC inhibitors, synthesis, biological evaluation, and molecular docking of novel Ugi products containing a zinc-chelating moiety are presented. One compound shows improved inhibitory potencies compared to SAHA, demonstrating that hindered lipophilic residues grafted on the peptide scaffold of the α-aminoacylamides can be favorable in the interaction with the enzyme.",

author = "Grolla, {Ambra A.} and Valeria Podest{\`a} and Chini, {Maria Giovanna} and {Di Micco}, Simone and Antonella Vallario and Genazzani, {Armando A.} and Canonico, {Pier Luigi} and Giuseppe Bifulco and Tron, {Gian Cesare} and Giovanni Sorba and Tracey Pirali",

year = "2009",

month = may,

day = "14",

doi = "10.1021/jm801529c",

language = "English",

volume = "52",

pages = "2776--2785",

journal = "Journal of Medicinal Chemistry",

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Grolla, AA, Podestà, V, Chini, MG, Di Micco, S, Vallario, A, Genazzani, AA, Canonico, PL, Bifulco, G, Tron, GC, Sorba, G & Pirali, T 2009, 'Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases', Journal of Medicinal Chemistry, vol. 52, n. 9, pagg. 2776-2785. https://doi.org/10.1021/jm801529c

Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases. / Grolla, Ambra A.; Podestà, Valeria; Chini, Maria Giovanna et al.
In: Journal of Medicinal Chemistry, Vol. 52, N. 9, 14.05.2009, pag. 2776-2785.

Risultato della ricerca: Contributo su rivista › Articolo in rivista › peer review

TY - JOUR

T1 - Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases

AU - Grolla, Ambra A.

AU - Podestà, Valeria

AU - Chini, Maria Giovanna

AU - Di Micco, Simone

AU - Vallario, Antonella

AU - Genazzani, Armando A.

AU - Canonico, Pier Luigi

AU - Bifulco, Giuseppe

AU - Tron, Gian Cesare

AU - Sorba, Giovanni

AU - Pirali, Tracey

PY - 2009/5/14

Y1 - 2009/5/14

N2 - HDAC inhibitors show great promise for the treatment of cancer. As part of a broader effort to explore the SAR of HDAC inhibitors, synthesis, biological evaluation, and molecular docking of novel Ugi products containing a zinc-chelating moiety are presented. One compound shows improved inhibitory potencies compared to SAHA, demonstrating that hindered lipophilic residues grafted on the peptide scaffold of the α-aminoacylamides can be favorable in the interaction with the enzyme.

AB - HDAC inhibitors show great promise for the treatment of cancer. As part of a broader effort to explore the SAR of HDAC inhibitors, synthesis, biological evaluation, and molecular docking of novel Ugi products containing a zinc-chelating moiety are presented. One compound shows improved inhibitory potencies compared to SAHA, demonstrating that hindered lipophilic residues grafted on the peptide scaffold of the α-aminoacylamides can be favorable in the interaction with the enzyme.

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U2 - 10.1021/jm801529c

DO - 10.1021/jm801529c

M3 - Article

SN - 0022-2623

VL - 52

SP - 2776

EP - 2785

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 9

ER -

Synthesis, biological evaluation, and molecular docking of Ugi products containing a zinc-chelating moiety as novel inhibitors of histone deacetylases

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