220129-77-1Relevant academic research and scientific papers
Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay
Rohe, Alexander,Goellner, Christiane,Wichapong, Kanin,Erdmann, Frank,Al-Mazaideh, Ghassab M.A.,Sippl, Wolfgang,Schmidt, Matthias
, p. 41 - 48 (2013/04/23)
In the human cell cycle, the Myt1 kinase is a crucial regulator of the G2/M transition. Because this membrane-associated kinase is hard to obtain and assay, there is a distinct lack of data so far. Here we report the derivatization of a glycoglycerolipid which was shown previously to be active in a Myt1 activity assay. These compounds were tested in a binding assay together with a set of common kinase inhibitors against a full-length Myt1 expressed in a human cell line. Dasatinib exhibited nanomolar affinity whereas broad coverage inhibitors such as sunitinib and staurosporine derivatives did not show any effect. We also carried out docking studies for the most potent compounds allowing further insights into the inhibitor interaction of this kinase. The glycoglycerolipids showed no significant effects in the binding assay, endorsing the idea of a mechanism of action distant from the active site.
Direct C-H amination of arenes with alkyl azides under rhodium catalysis
Shin, Kwangmin,Baek, Yunjung,Chang, Sukbok
, p. 8031 - 8036 (2013/08/23)
New horizons in the utility of azides: The rhodium-catalyzed intermolecular direct C-H amination of arenes with alkyl azides provides a convenient route to N-alkyl anilines (see scheme; DG=directing group). Alkyl azides with a wide range of functional groups reacted readily with various substrates, including benzamides, aromatic ketones, and flavones. Copyright
A focused sulfated glycoconjugate Ugi library for probing heparan sulfate-binding angiogenic growth factors
Liu, Ligong,Li, Caiping,Cochran, Siska,Feder, Daniel,Guddat, Luke W.,Ferro, Vito
supporting information, p. 6190 - 6194 (2012/10/29)
A library of small molecule heparan sulfate (HS) mimetics was synthesized by employing the Ugi four-component condensation of d-mannopyranoside-derived isocyanides with formaldehyde as the carbonyl component and a selection of carboxylic acids and amines,
Towards a stable noeuromycin analog with a d-manno configuration: Synthesis and glycosidase inhibition of d-manno-like tri- and tetrahydroxylated azepanes
Deschamp, Julia,Mondon, Martine,Nakagawa, Shinpei,Kato, Atsushi,Alonzi, Dominic S.,Butters, Terry D.,Zhang, Yongmin,Sollogoub, Matthieu,Blériot, Yves
, p. 641 - 649 (2012/03/11)
Noeuromycin is a highly potent albeit unstable glycosidase inhibitor due to its hemiaminal function. While stable d-gluco-like analogs have been reported, no data are available for d-manno-like structures. A series of tri- and tetrahydroxylated seven-memb
Synthesis of analogs of 1,1-linked galactosyl mannoside as mimetics of sialyl Lewis X tetrasaccharide
Hiruma, Kazumi,Kanie, Osamu,Wong, Chi-Huey
, p. 15781 - 15792 (2007/10/03)
Methods have been developed for the incorporation of hydrophobic groups with and without positive or negative charge to position-6 of the mannose residue in the 1,1-linked disaccharide as mimetics of sialyl Lewis X tetrasaccharide in order to enhance binding affinity to selectins.
