- Design, synthesis and in vitro evaluation of 6-amide-2-aryl benzoxazole/benzimidazole derivatives against tumor cells by inhibiting VEGFR-2 kinase
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Herein, we have carried out a structural optimization campaign to discover the novel anti-tumor agents with our previously screened YQY-26 as the hit compound. A library of thirty-seven 6-amide-2-aryl benzoxazole/benzimidazole derivatives has been designe
- Yuan, Xu,Yang, Qingyi,Liu, Tongyan,Li, Ke,Liu, Yuwen,Zhu, Changcheng,Zhang, Zhiyun,Li, Linghua,Zhang, Conghai,Xie, Mingjin,Lin, Jun,Zhang, Jihong,Jin, Yi
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p. 147 - 165
(2019/06/27)
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- Expanding Benzoxazole-Based Inosine 5′-Monophosphate Dehydrogenase (IMPDH) Inhibitor Structure-Activity As Potential Antituberculosis Agents
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New drugs and molecular targets are urgently needed to address the emergence and spread of drug-resistant tuberculosis. Mycobacterium tuberculosis (Mtb) inosine 5′-monophosphate dehydrogenase 2 (MtbIMPDH2) is a promising yet controversial potential target
- Chacko, Shibin,Boshoff, Helena I. M.,Singh, Vinayak,Ferraris, Davide M.,Gollapalli, Deviprasad R.,Zhang, Minjia,Lawson, Ann P.,Pepi, Michael J.,Joachimiak, Andrzej,Rizzi, Menico,Mizrahi, Valerie,Cuny, Gregory D.,Hedstrom, Lizbeth
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p. 4739 - 4756
(2018/05/23)
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- Synthesis, molecular docking and antimicrobial evaluation of novel benzoxazole derivatives
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In this research, previously and newly synthesized 5-amino-2-(4-substitutedphenyl/benzyl)benzoxazoles (3a-3l) and 2-substituted-5-(4-nitro/aminophenylsulfonamido)benzoxazoles (5a-5l, 6a-6l) were evaluated for their antimicrobial activities against Pseudom
- Ertan-Bolelli, Tugba,Yildiz, Ilkay,Ozgen-Ozgacar, Selda
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p. 553 - 567
(2016/03/08)
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- Metallomesogens derived from benzoxazoles-salicylaldimine conjugates
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The synthesis, characterization, and mesomorphic properties of a new series of Schiff bases 2a-h and metal complexes 1a-h-M are prepared and their mesomorphic properties studied. Two single crystallographic structures of 2d (n=12, m=1) and 1g-Pd (n=m=12) were determined by X-ray analysis. Both compounds crystallize in a triclinic space group P-1. A dimeric structure formed by intermolecular H-bonds in 2d was observed, giving nematic phase due to a better aspect ratio. The central geometry at Pd2+ ion is nearly perfect square plane. All Schiff bases 2a-h formed N or/and SmC phases. The formation of mesophases of complexes 1a-h-M was strongly dependent on metal ions incorporated. All Cu2+, Ni2+ and Pd2+ complexes exhibited N or/and SmC phase, respectively. However, Zn2+ and Co2+ complexes were not mesogenic. The lack of mesomorphism was probably attributed to a preferred tetrahedral geometry at Zn2+ and Co2+ over a square-planar geometry at Cu2+ and Pd 2+.
- Chen, Chun-Jung,Wang, I-Wen,Sheu, Hwo-Shuenn,Lee, Gene-Hsiang,Lai, Chung K.
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p. 8120 - 8130
(2011/10/31)
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- Discovery of 2-arylbenzoxazoles as upregulators of utrophin production for the treatment of duchenne muscular dystrophy
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Figure Presented. A series of novel 2-arylbenzoxazoles that upregulate the production of utrophin in murine H2K cells, as assessed using a luciferase reporter linked assay, have been identified. This compound class appears to hold considerable promise as a potential treatment for Duchenne muscular dystrophy. Following the delineation of structure-activity relationships in the series, a number of potent upregulators were identified, and preliminary ADME evaluation is described. These studies have resulted in the identification of 1, a compound that has been progressed to clinical trials.
- Chancellor, Daniel R.,Davies, Kay E.,De Moor, Olivier,Dorgan, Colin R.,Johnson, Peter D.,Lambert, Adam G.,Lawrence, Daniel,Lecci, Cristina,Maillol, Carole,Middleton, Penny J.,Nugent, Gary,Poignant, Séverine D.,Potter, Allyson C.,Price, Paul D.,Pye, Richard J.,Storer, Richard,Tinsley, Jonathon M.,Van Well, Renate,Vickers, Richard,Vile, Julia,Wilkes, Fraser J.,Wilson, Francis X.,Wren, Stephen P.,Wynne, Graham M.
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supporting information; experimental part
p. 3241 - 3250
(2011/07/06)
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