- A concise synthesis of 2,4-disubstituted pyridines: A convenient synthesis of 2-bromo-4-iodopyridine via halogen dance and its successive one-pot disubstitutions
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As a key building block for 2,4-disubstituted pyridines, 2-bromo-4-iodopyridine was synthesized conveniently from 2-bromopyridine using LDA and I2 via 'halogen dance'. 2-Bromo-4-iodopyridine was then converted to other 2,4-diaryl pyridines and
- Duan, Xin-Fang,Li, Xiang-Hong,Li, Fu-You,Huang, Chun-Hui
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- Regioselectivity in alkenyl(aryl)-heteroaryl Suzuki cross-coupling reactions of 2,4-dibromopyridine. A?synthetic and mechanistic study
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2,4-Dibromopyridine undergoes a regioselective Suzuki cross-coupling reaction at position 2 with several alkenyl(aryl) boronic acids to render 4-bromo-2-carbon substituted pyridines, difficult to be prepared otherwise, in good yields under palladium catal
- Sicre, Cristina,Alonso-Gómez, J.-Lorenzo,Cid, M. Magdalena
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- A Dichotomy in Cross-Coupling Site Selectivity in a Dihalogenated Heteroarene: Influence of Mononuclear Pd, Pd Clusters, and Pd Nanoparticles-The Case for Exploiting Pd Catalyst Speciation
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Site-selective dihalogenated heteroarene cross-coupling with organometallic reagents usually occurs at the halogen proximal to the heteroatom, enabled by intrinsic relative electrophilicity, particularly in strongly polarized systems. An archetypical exam
- Eyles, Anthony,Fairlamb, Ian J. S.,Ford, Mark J.,Jeddi, Neda,Scott, Neil W. J.,Simon, Lauriane,Tanner, Theo,Whitwood, Adrian C.,Willans, Charlotte E.
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supporting information
p. 9682 - 9693
(2021/07/19)
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- Structure-Activity Relationship Study of Novel 6-Aryl-2-benzoyl-pyridines as Tubulin Polymerization Inhibitors with Potent Antiproliferative Properties
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We recently reported the crystal structure of tubulin in complex with a colchicine binding site inhibitor (CBSI), ABI-231, having 2-aryl-4-benzoyl-imidazole (ABI). Based on this and additional crystal structures, here we report the structure-activity relationship study of a novel series of pyridine analogues of ABI-231, with compound 4v being the most potent one (average IC50 ~1.8 nM) against a panel of cancer cell lines. We determined the crystal structures of another potent CBSI ABI-274 and 4v in complex with tubulin and confirmed their direct binding at the colchicine site. 4v inhibited tubulin polymerization, strongly suppressed A375 melanoma tumor growth, induced tumor necrosis, disrupted tumor angiogenesis, and led to tumor cell apoptosis in vivo. Collectively, these studies suggest that 4v represents a promising new generation of tubulin inhibitors.
- Chen, Hao,Deng, Shanshan,Wang, Yuxi,Albadari, Najah,Kumar, Gyanendra,Ma, Dejian,Li, Weimin,White, Stephen W.,Miller, Duane D.,Li, Wei
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p. 827 - 846
(2020/02/04)
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- A facile synthesis of 4-Ar-2-bromopyridine and its 2,2′-bipyridine derivatives
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By means of selective cross-coupling of ArMgBr with 2-bromo-4-iodopyridine in the presence of a catalytic amount of Pd(PPh3)4, 4-Ar-2-bromopyridines were facilely one-step synthesized. These pyridine compounds were smoothly transform
- Duan, Xin-Fang,Li, Xiang-Hong,Li, Fu-You,Huang, Chun-Hui
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p. 3227 - 3233
(2007/10/03)
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- Synthese de composes macrocycliques comportant deux fragments coordinants separes et differents, de type bipyridyl-2,2' et diphenyl-2,9 phenanthroline-1,10.
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Macrocyclic compounds containing a 2,9-diphenyl-1,10-phenanthroline subunit and a peripheral 2,2'-bipyridine chelate have been synthesized.In compound 4, the links between both coordinating fragments are flexible enough to allow complete folding of the molecule during complexation whereas in 5, the complexing moieties are rigidly held apart and cannot bind to the same metallic center.
- Chambron, Jean-Claude,Sauvage, Jean-Pierre
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p. 895 - 904
(2007/10/02)
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