908859-97-2Relevant academic research and scientific papers
Highly potent and selective histone deacetylase 6 inhibitors designed based on a small-molecular substrate
Suzuki, Takayoshi,Kouketsu, Akiyasu,Itoh, Yukihiro,Hisakawa, Shinya,Maeda, Satoko,Yoshida, Minoru,Nakagawa, Hidehiko,Miyata, Naoki
, p. 4809 - 4812 (2006)
To find novel histone deacetylase 6 (HDAC6)-selective inhibitors and clarify the structural requirements for HDAC6-selective inhibition, we prepared thiolate analogues designed based on the structure of an HDAC6-selective substrate and evaluated the histo
NEW THIO DERIVATIVES BEARING LACTAMS AS POTENT HDAC INHIBITORS AND THEIR USES AS MEDICAMENTS
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Page/Page column 0184; 0185; 0186; 0187; 0188, (2014/07/23)
The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an i
ST7612AA1, a thioacetate-ω(γ-lactam carboxamide) derivative selected from a novel generation of oral HDAC inhibitors
Barbarino, Marcella,Battistuzzi, Gianfranco,Cabri, Walter,Fant, Nicola,Giannini, Giuseppe,Guglielmi, Mario Berardino,Milazzo, Ferdinando M.,Mor, Marco,Pala, Daniele,Pisano, Claudio,Rivara, Silvia,Santaniello, Mos,Taddei, Maurizio,Vesci, Loredana,Vignola, Davide
, p. 8358 - 8377 (2014/12/11)
A systematic study of medicinal chemistry aimed at identifying a new generation of HDAC inhibitors, through the introduction of a thiol zinc-binding group (ZBG) and of an amide-lactam in the ω-position of the polyethylene chain of the vorinostat scaffold,
NEW THIO DERIVATIVES BEARING LACTAMS AS POTENT HDAC INHIBITORS AND THEIR USES AS MEDICAMENTS
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Page/Page column 25; 26, (2013/04/10)
The present invention relates to novel amide compounds of Formula (I), and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an i
Design, synthesis, structure-selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors
Itoh, Yukihiro,Suzuki, Takayoshi,Kouketsu, Akiyasu,Suzuki, Nobuaki,Maeda, Satoko,Yoshida, Minoru,Nakagawa, Hidehiko,Miyata, Naoki
, p. 5425 - 5438 (2008/03/14)
To uncover novel histone deacetylase 6 (HDAC6)-selective inhibitors and to elucidate the structural requirements for their inhibitory activity, we designed and prepared a series of thiolate analogues based on the structure of an HDAC6-selective substrate and evaluated their properties by Western blotting and enzyme assays. Several thiolate analogues were found to be potent and selective HDAC6 inhibitors. Study of the structure-selectivity relationship revealed that the presence of a bulky alkyl group and tert-butylcarbamate group in these compounds is important for HDAC6-selective inhibition. Compounds 16b and 20b, the most selective and active compounds in this series, exerted a synergistic inhibition of cancer cell growth in combination with paclitaxel. They also blocked the growth of estrogen receptor α-positive breast cancer MCF-7 cells that had been treated with estrogen. These findings suggested that HDAC6-selective inhibitors have potential as anticancer agents.
