202805-07-0Relevant articles and documents
Synthesis of 2′-amino-2′-deoxyuridine modified by 1,8-naphthalimide
Li, Heting,Jiang, Zhiqin,Wang, Xin,Zheng, Chao
, p. 1933 - 1940 (2006)
A simple and efficient synthetic route of 2′-amino-2′- deoxyuridine was studied. 2′-Amino-2′-deoxyuridine was incorporated into 1,8-naphthalimides in the 2′-position of 2′-sugar via linking arms of different lengths. A convenient method for the synthesis of the conjugates was adopted. Copyright Taylor & Francis Group, LLC.
A fluorescent histone deacetylase (HDAC) inhibitor for cellular imaging
Fleming, Cassandra L.,Ashton, Trent D.,Nowell, Cameron,Devlin, Mark,Natoli, Anthony,Schreuders, Jeannette,Pfeffer, Frederick M.
, p. 7827 - 7830 (2015)
Fluorescence microscopy studies using 4-morpholinoscriptaid (4MS) demonstrated rapid cellular uptake of this scriptaid analogue into the cytoplasm but no nuclear penetration. As 4MS and scriptaid have the same in vitro activity against HDACs and KASUMI-1 cells; 4MS exemplifies a rational approach to subtly modify 'profluorogenic' substrates for intracellular studies.
Highly fluorescent and HDAC6 selective scriptaid analogues
Fleming, Cassandra L.,Natoli, Anthony,Schreuders, Jeannette,Devlin, Mark,Yoganantharajah, Prusothman,Gibert, Yann,Leslie, Kathryn G.,New, Elizabeth J.,Ashton, Trent D.,Pfeffer, Frederick M.
supporting information, p. 321 - 333 (2018/11/24)
Fluorescent scriptaid analogues with excellent HDAC6 selectivity (HDAC1/6 > 500) and potency (HDAC6 IC50 F = 0.83 in DMSO and 0.38 in aqueous buffer) makes them ideally suited for cellular imaging and visualisation of their cytoplasmic localisation was readily accomplished. Whole organism imaging in zebrafish confirmed both the vascular localisation of the new inhibitors and the impact of HDAC6 inhibition on in vivo development.
Synthesis and modification of terrylenediimides as high-performance fluorescent dyes
Nolde, Fabian,Qu, Jianqiang,Kohl, Christopher,Pschirer, Neil G.,Reuther, Erik,Muellen, Klaus
, p. 3959 - 3967 (2007/10/03)
Two new synthetic approaches to terrylenediimides, highly photostable fluorescent dyes, are described. For the first time terrylenediimide has been synthesised in a straightforward procedure that makes large quantities available. The second route includes an efficient cross-coupling reaction followed by a cyclodehy-drogenation. Monofunctionalisation of the imide structure allows terrylenediimides now to be coupled with a variety of compounds, for example, by Suzuki cross-coupling, which can lead to an array of terrylenediimides with new functional groups such as hydroxy, amino, or carboxy groups needed to link up with other molecules. The functionalisation in the bay region is used to tune the properties of terrylenediimides and extend the range of applications, for example, by introducing water solubility. These tetrasubstituted terrylenediimides offer, depending on the substituents used, exciting features such as good solubility in common organic solvents, water solubility, or NIR absorption.
(2-Amino-phenyl)-amides of ω-substituted alkanoic acids as new histone deacetylase inhibitors
Vaisburg, Arkadii,Bernstein, Naomy,Frechette, Sylvie,Allan, Martin,Abou-Khalil, Elie,Leit, Silvana,Moradei, Oscar,Bouchain, Giliane,Wang, James,Woo, Soon Hyung,Fournel, Marielle,Yan, Pu T.,Trachy-Bourget, Marie-Claude,Kalita, Ann,Beaulieu, Carole,Li, Zuomei,MacLeod, A. Robert,Besterman, Jeffrey M.,Delorme, Daniel
, p. 283 - 287 (2007/10/03)
A variety of ω-substituted alkanoic acid (2-amino-phenyl)-amides were designed and synthesized. These compounds were shown to inhibit recombinant human histone deacetylases (HDACs) with IC50 values in the low micromolar range and induce hyperacetylation of histones in whole cells. They induced expression of p21WAF1/Cip1 and caused cell-cycle arrest in human cancer cells. Compounds in this class showed efficacy in human tumor xenograft models.
