- Synthesis and biological evaluation of prodrugs for nitroreductase based 4-β-amino-4′-Demethylepipodophyllotoxin as potential anticancer agents
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A series of prodrugs for nitroreductase (NTR) based 4-β-amino-4′- Demethylepipodophyllotoxin as potential anticancer agents were synthesized, and their antiproliferative activities in vitro showed compounds 2b (IC50 = 0.77, 0.83 and 1.19 μM) an
- Deng, Wei,He, Dian,Wu, Zheng-Rong
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- Quantitative helix handedness bias through a single Hvs.CH3stereochemical differentiation
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A novel chiral aromatic δ-amino acid building block was shown to fully induce handedness in quinoline oligoamide foldamers with the possibility of further increasing the bias by combining multiples of these units in the same sequence. Through its incorporation within the helix, both N- and C-termini are still accessible for further functionalisation.
- Bindl, Daniel,Heinemann, Elisabeth,Mandal, Pradeep K.,Huc, Ivan
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supporting information
p. 5662 - 5665
(2021/06/16)
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- Synthesis and herbicidal activities of aryloxyacetic acid derivatives as HPPD inhibitors
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A series of aryloxyacetic acid derivatives were designed and synthesized as 4-hydoxyphenylpyruvate dioxygenase (HPPD) inhibitors. Preliminary bioassay results reveal that these derivatives are promising Arabidopsis thaliana HPPD (AtHPPD) inhibitors, in particular compounds I12 (Ki = 0.011 μM) and I23 (Ki = 0.012 μM), which exhibit similar activities to that of mesotrione, a commercial HPPD herbicide (Ki = 0.013 μM). Furthermore, the newly synthesized compounds show significant greenhouse herbicidal activities against tested weeds at dosages of 150 g ai/ha. In particular, II4 exhibited high herbicidal activity for pre-emergence treatment that was slightly better than that of mesotrione. In addition, compound II4 was safe for weed control in maize fields at a rate of 150 g ai/ha, and was identified as the most potent candidate for a novel HPPD inhibitor herbicide. The compounds described herein may provide useful guidance for the design of new HPPD inhibiting herbicides and their modification.
- Huang, Hao,Liu, Jian-Min,Shu, Lei,Wang, Man-Man,Yan, Yi-Le,Zhang, Da-Yong,Zhang, Jian-Qiu
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supporting information
p. 233 - 247
(2020/03/27)
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- Deconstructive di-functionalization of unstrained, benzo cyclic amines by C-N bond cleavage using a recyclable tungsten catalyst
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With H2WO4 as the catalyst and H2O2 as the oxidant, we herein report a deconstructive difunctionalization of the C-N bond in unstrained, benzo cyclic amines to generate an ester group and nitro group simultaneously. The preliminary mechanistic studies suggested that the corresponding hydroxamic acid is the key intermediate for this transformation. Importantly, with the utilization of this transformation, we achieved an interesting approach for the ring contraction of quinoline to indole, an example of scaffold hopping in a hetero-aromatic system.
- Zhang, Yujing,Sun, Shuai,Su, Yijin,Zhao, Jian,Li, Yong-Hong,Han, Bo,Shi, Feng
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supporting information
p. 4970 - 4974
(2019/05/29)
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- Reductive cyclizations of nitroarenes to hydroxamic acids by visible light photoredox catalysis
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We have developed a photocatalytic reduction of nitroarenes as an efficient, chemoselective route to biologically important N-phenyl hydroxamic acid scaffolds. Optimal conditions call for 2.5 mol% of a ruthenium photocatalyst, visible light irradiation, and a dihydropyridine terminal reductant. Because of the mild nature of the visible light activation, functional groups that might be sensitive to other non-photochemical reduction methods are easily tolerated. Georg Thieme Verlag Stuttgart New York.
- Cismesia, Megan A.,Ischay, Michael A.,Yoon, Tehshik P.
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supporting information
p. 2699 - 2705
(2013/10/21)
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- Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose) polymerase inhibitors
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Structure based drug design of a series of novel 1,4-benzoxazin-3-one derived PARP-1 inhibitors are described. The synthesis, enzymatic & cellular activities and pharmacodynamic effects are described. Optimized analogs demonstrated inhibition of poly-ADP-ribosylation in SW620 tumor bearing nude mice through 24 h following a single dose.
- Gangloff, Anthony R.,Brown, Jason,De Jong, Ron,Dougan, Douglas R.,Grimshaw, Charles E.,Hixon, Mark,Jennings, Andy,Kamran, Ruhi,Kiryanov, Andre,O'Connell, Shawn,Taylor, Ewan,Vu, Phong
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supporting information
p. 4501 - 4505
(2013/08/15)
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- Aza-Michael addition of acrylonitrile with 2-aryloxymethylbenzimidazole derivatives under microwave irradiation
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A simple, rapid, and highly efficient method has been developed for the aza-Michael addition of acrylonitrile to 2-aryl-oxymethylbenzimidazole derivatives in the presence of anhydrous potassium carbonate under microwave irradiation. A series novel of 1-cyanoethyl-2-aryloxymethylbenzimidazole derivatives have been prepared and characterised by 1H NMR, 13C NMR, IR spectra and elemental analysis.
- Wei, Tai-Bao,Hua, Mao-Tang,Shi, Hai-Xiong,Liu, Yong,Zhang, You-Ming
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scheme or table
p. 452 - 454
(2010/12/24)
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- Palladium-catalyzed C-O bond formation: direct synthesis of phenols and aryl/alkyl ethers from activated aryl halides
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A simple and efficient palladium-catalyzed carbon-oxygen bond formation is reported. The palladium-tri-tert-butylphosphine complex was found to be effective in converting haloarenes to corresponding substituted phenols. This methodology offers a direct transformation of aryl halides to phenols, as well as the straightforward application to generate a wide variety of diaryl or alkyl/aryl ethers.
- Chen, Guoshu,Chan, Albert S.C.,Kwong, Fuk Yee
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p. 473 - 476
(2008/02/03)
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- A rapid and high-yield synthesis of aryloxyacetic acid in one pot under microwave irradiation and phase transfer catalysis conditions
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A series of aryloxyacetic acid 3a-h has been synthesized in one pot under microwave irradiation and phase transfer catalysis conditions. By the optimization of the reaction condition, a rapid, high-yield and efficient method for the preparation of aryloxyacetic acid is reported.
- Wei, Tai-Bao,Liu, Hong,Li, Man-Lin,Zhang, You-Ming
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p. 1312 - 1314
(2007/10/03)
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- Rapid and high-yield synthesis of aryloxyacetates under microwave irradiation and phase-transfer catalysis conditions
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A series of methyl aryloxyacetates (3a-3f) have been synthesized by the reaction of substituted phenol with methyl chloroacetate under the conditions of microwave irradiation and phase-transfer catalysis. By the optimization of the reaction conditions, we developed a good method for the preparation of methyl aryloxyacetates, which have the advantages of high yields, short reaction times, ease of workup, and simple operation. Copyright Taylor & Francis, Inc.
- Wei, Tai-Bao,Liu, Hong,Li, Man-Lin,Zhang, You-Ming
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p. 1759 - 1764
(2007/10/03)
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- A rapid and high-yield synthesis of aryloxyacetyl hydrazides under microwave irradiation and with phase transfer catalysis
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A series of aryloxyacetyl hydrazides 4a-l were synthesised under microwave irradiation and phase transfer catalysis conditions. By the optimisation of the reaction conditions, a rapid, high-yield and efficient method for the preparation of aryloxyacety hydrazide was given.
- Wei, Tai-Bao,Liu, Hong,Li, Man-Lin,Zhang, You-Ming
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p. 432 - 433
(2007/10/03)
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- Applicability of Hammett Equation to Kinetics of Acid-catalysed Esterification of ortho-Substituted Phenoxyacetic, Phenylmercaptoacetic and Phenylsulphonylacetic Acids by Methanol
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Correlation analysis of the title rate data shows that the steric effects of ortho-substituents are absent at the reaction centre.
- Baliah, V.,Gurumurthy, R.
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p. 257 - 258
(2007/10/02)
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- Applicability of Hammett Equation to Insulated Systems - Kinetics of Alkaline Hydrolysis of ortho-Substituted Methyl Phenoxyacetates
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Kinetics of alkaline hydrolysis of some ortho-substituted methyl phenoxyacetates in methanol-water (85percent wt/wt) at 10 deg, 15 deg and 20 deg are reported.The application of Taft's steric energy relationship shows that the reaction is not susceptible
- Gurumurthy, R.,Balakrishnan, N.
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p. 1114 - 1115
(2007/10/02)
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