- Incorporation of histone deacetylase inhibitory activity into the core of tamoxifen – A new hybrid design paradigm
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Hybrid antiestrogen/histone deacetylase (HDAC) inhibitors were designed by appending zinc binding groups to the 4-hydroxystilbene core of 4-hydroxytamoxifen. The resulting hybrids were fully bifunctional, and displayed high nanomolar to low micromolar IC
- Palermo, Anthony F.,Diennet, Marine,El Ezzy, Mohamed,Williams, Benjamin M.,Cotnoir-White, David,Mader, Sylvie,Gleason, James L.
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supporting information
p. 4428 - 4440
(2018/08/06)
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- Aryl ethynyl anthraquinones: A useful platform for targeting telomeric G-quadruplex structures
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Aryl ethynyl anthraquinones have been synthesized by Sonogashira cross-coupling and evaluated as telomeric G-quadruplex ligands, by the FRET melting assay, circular dichroism, the DNA synthesis arrest assay and molecular docking. Both the binding properti
- Percivalle, Claudia,Sissi, Claudia,Greco, Maria Laura,Musetti, Caterina,Mariani, Angelica,Artese, Anna,Costa, Giosuè,Perrore, Maria Lucia,Alcaro, Stefano,Freccero, Mauro
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supporting information
p. 3744 - 3754
(2014/06/09)
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- Synthesis and growth inhibition activity of fluorinated derivatives of tamoxifen
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The design and synthesis of 11 fluorinated derivatives of tamoxifen are described. Growth inhibition values (GI50) on human HT-29, M21, MCF7, and MDA-MB-231 tumor cells are also reported. In general, the GI50 values are similar or sl
- Malo-Forest, Bianca,Landelle, Grégory,Roy, Jessye-Ann,Lacroix, Jacques,Gaudreault, René C.,Paquin, Jean-Fran?ois
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p. 1712 - 1715
(2013/03/29)
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- STRUCTURE, SYNTHESIS, AND APPLICATIONS FOR OLIGO PHENYLENE ETHYNYLENES (OPES)
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The present disclosure provides novel oligo phenylene ethynylene (OPE) compounds, methods for synthesizing these compounds, and materials and substances incorporating these compounds. The various OPEs show antibacterial, antiviral and antifungal activity.
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Page/Page column 3; 9
(2012/02/02)
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- Zirconocene-mediated highly regio- and stereoselective synthesis of multisubstituted olefins starting from 1-alkynylboronates
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Multisubstituted olefins are efficiently prepared by the zirconocene-mediated regio- and stereoselective coupling between 1-alkynylboronates and ethylene, followed by sequential transformation in moderate to high yields. The proper combination of substrates and reaction conditions is important for high yields. The synthesis of various tetrasubstituted alkenes in a regio- and stereocontrolled manner is described. This methodology has been applied to the synthesis of (Z)-tamoxifen in a concise, regio- and stereoselective manner. This multicomponent coupling strategy involves the characteristics of 1-alkynylboronates toward high selectivities followed by palladium(0)-mediated cross-coupling with aryl halides. Copyright
- Nishihara, Yasushi,Miyasaka, Mitsuru,Okamoto, Masanori,Takahashi, Hideki,Inoue, Eiji,Tanemura, Kenki,Takagi, Kentaro
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p. 12634 - 12635
(2008/03/13)
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- Effective synthesis of tamoxifen using nickel-catalyzed arylative carboxylation
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Tamoxifen was synthesized using a nickel-catalyzed arylative carboxylation developed by our group. The key compound, tetrasubstituted alkene, was synthesized from disubstituted alkyne using a catalytic amount of Ni(0) and DBU in the presence of Ph2Zn under an atmosphere of carbon dioxide. The reaction proceeded smoothly in a regio- and stereoselective manner, and the resultant tetrasubstituted alkene was converted into tamoxifen. Georg Thieme Verlag Stuttgart.
- Shimizu, Kazuya,Takimoto, Masanori,Mori, Miwako,Sato, Yoshihiro
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p. 3182 - 3184
(2008/02/13)
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- NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES
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The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen at
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Page/Page column 129
(2008/06/13)
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- PHENYLPYRIDINE CARBONYL PIPERAZINE DERIVATIVE
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The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (whereinR1, R2: hydrogen, a halogen, a lower alkyl, a lower alkoxy, or the like,R3, R4: hydrogen, a (substituted) lower alkyl, a halogen, or the like,R5: hydrogen, a lower alkyl, a lower alkoxycarbonyl, or the like, andn: 0 or 1).
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- (Z)-tamoxifen and tetrasubstituted alkenes and dienes via a regio- and stereospecific three-component magnesium carbometalation palladium(O) cross-coupling strategy
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(Matrix presented) The synthesis of various tetrasubstituted alkenes and dienes in a regio- and stereocontrolled manner is described. This three-component coupling strategy involves the addition of Grignard reagents to propargyl alcohols followed by palladium(O)-mediated cross-coupling with aryl or vinyl halides. This protocol has been applied to the synthesis of (Z)-Tamoxifen and related mimics.
- Tessier, Pierre E.,Penwell, Andrea J.,Souza, Fabio E. S.,Fallis, Alex G.
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p. 2989 - 2992
(2007/10/03)
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- Stereospecific synthesis of clomiphene and tamoxifen via stannylcupration of diphenylacetylene
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Stereospecific trans-stannylcupration of diphenylacetylene affords a 1,2-dimetallostilbene which may be elaborated into either Clomiphene or Tamoxifen through palladium-catalyzed coupling with an aryl iodide.
- Cummins
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p. 4071 - 4079
(2007/10/03)
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