13807-10-8Relevant academic research and scientific papers
Traceless solid-phase synthesis of 2,4,5-trisubstituted thiazoles
Lee, Ill Young,Lee, Jin Young,Lee, Hye Jin,Gong, Young-Dae
, p. 2483 - 2485 (2005)
The solid-phase synthesis of trisubstituted thiazoles is described. The synthetic strategy involves the formation of a polymer-bound thiazole by reacting resin-bound cyanodithioimidocarbonic acid and α-bromoketone. The resin-bound thiazole was reacted with acyl chlorides or isocyanates. After oxidation-activation of a thioether linker to a sulfone linker, traceless cleavage was achieved with nucleophiles to give trisubstituted thiazoles. Georg Thieme Verlag Stuttgart.
DIAMINOTHIAZOLE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
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Paragraph 00163; 00164; 00165, (2018/05/27)
The disclosure relates to diaminothiazole derivatives of formula (I) where the variables are as defined herein, pharmaceutical compositions containing such compounds, and methods for the use of such compounds and compositions for the treatment of hyperpro
Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases
Schonbrunn, Ernst,Betzi, Stephane,Alam, Riazul,Martin, Mathew P.,Becker, Andreas,Han, Huijong,Francis, Rawle,Chakrasali, Ramappa,Jakkaraj, Sudhakar,Kazi, Aslamuzzaman,Sebti, Said M.,Cubitt, Christopher L.,Gebhard, Anthony W.,Hazlehurst, Lori A.,Tash, Joseph S.,Georg, Gunda I.
, p. 3768 - 3782 (2013/06/27)
Cyclin-dependent kinases (CDKs) are serine/threonine protein kinases that act as key regulatory elements in cell cycle progression. We describe the development of highly potent diaminothiazole inhibitors of CDK2 (IC50 = 0.0009-0.0015 μM) from a
From on-target to off-target activity: Identification and optimisation of Trypanosoma brucei GSK3 inhibitors and their characterisation as anti-Trypanosoma brucei drug discovery lead molecules
Woodland, Andrew,Grimaldi, Raffaella,Luksch, Torsten,Cleghorn, Laura A. T.,Ojo, Kayode K.,VanVoorhis, Wesley C.,Brenk, Ruth,Frearson, Julie A.,Gilbert, Ian H.,Wyatt, Paul G.
, p. 1127 - 1137 (2013/07/26)
Human African trypanosomiasis (HAT) is a life-threatening disease with approximately 30000-40000 new cases each year. Trypanosoma brucei protein kinase GSK3 short (TbGSK3) is required for parasite growth and survival. Herein we report a screen of a focused kinase library against T.brucei GSK3. From this we identified a series of several highly ligand-efficient TbGSK3 inhibitors. Following the hit validation process, we optimised a series of diaminothiazoles, identifying low-nanomolar inhibitors of TbGSK3 that are potent invitro inhibitors of T.brucei proliferation. We show that the TbGSK3 pharmacophore overlaps with that of one or more additional molecular targets.
One-pot sequential multicomponent route to 2,4-diaminothiazoles - A facile approach to bioactive agents for cancer therapeutics
Sreejalekshmi, Kumaran G.,Rajasekharan, Kallikat N.
, p. 3627 - 3629 (2012/09/22)
A facile one-pot sequential three-component route to 2,4-diaminothiazoles is reported. The new approach employs the mildest reaction conditions and commercially available reagents to generate diverse 2-alkyl/arylamino-4-amino-5- aroyl/heteroylthiazoles in short reaction times, good yield, and purity.
2-Arylamino-4-amino-5-aroylthiazoles. "One-pot" synthesis and biological evaluation of a new class of inhibitors of tubulin polymerization
Romagnoli, Romeo,Baraldi, Pier Giovanni,Carrion, Maria Dora,Cruz-Lopez, Olga,Cara, Carlota Lopez,Basso, Giuseppe,Viola, Giampietro,Khedr, Mohammed,Balzarini, Jan,Mahboobi, Siavosh,Sellmer, Andreas,Brancale, Andrea,Hamel, Ernest
supporting information; experimental part, p. 5551 - 5555 (2010/02/28)
The essential role of microtubules in mitosis makes them a major target of compounds useful for cancer therapy. In our search for potent antitumor agents, a novel series of 2-anilino-4-amino-5-aroylthiazoles was synthesized and evaluated for antiprolifera
An efficient protocol for solid phase aminothiazole synthesis
Sreejalekshmi, Kumaran G.,Devi, Satyabhama K.C.,Rajasekharan, Kallikat N.
, p. 6179 - 6182 (2007/10/03)
An efficient synthesis of 2,4-diamino-5-ketothiazoles under solid phase conditions has been achieved by the reaction of polymer supported amidinothioureas with α-haloketones. This novel synthetic approach involving traceless cleavage from the support is s
PDE4B inhibitors and uses therefor
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Page/Page column 47-48, (2008/06/13)
Compounds active on phosphodiesterase PDE4B are provided. Also provided herewith are compositions useful for treatment of PDE4B-mediated diseases or conditions, and methods for the use thereof.
Inhibitors of glycogen synthase kinase-3 (gsk-3) for treating glaucoma
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, (2008/06/13)
The use of inhibitors of GSK-3 useful for treating glaucoma is disclosed.
