Org. and Biomol. Chem.

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RSC - Org. Biomol. Chem. latest articles
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Aliphatic acid-conjugated antimicrobial peptides - potential agents with anti-tumor, multidrug resistance-reversing activity and enhanced stability

16 July, 2015 - 02:54

Org. Biomol. Chem., 2015, 13,7673-7680
DOI: 10.1039/C5OB00752F, PaperXin Deng, Qianqian Qiu, Ke Ma, Xuekun Wang, Wenlong Huang, Hai Qian
We have designed and synthesized a series of aliphatic acid-conjugated peptides. Biological evaluation revealed that these peptides showed improved anti-tumor activity, plasma stability over the lead compound, and also multidrug resistance-reversing effects on multidrug-resistant cells.
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Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold

16 July, 2015 - 02:54

Org. Biomol. Chem., 2015, 13,7643-7654
DOI: 10.1039/C5OB00778J, PaperJian Liu, Xia Peng, Yang Dai, Wei Zhang, Sumei Ren, Jing Ai, Meiyu Geng, Yingxia Li
Fibroblast growth factor receptor (FGFR) is a potential target for cancer therapy.
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Investigation of the active turn geometry for the labour delaying activity of indolizidinone and azapeptide modulators of the prostaglandin F2[small alpha] receptor

16 July, 2015 - 02:54

Org. Biomol. Chem., 2015, 13,7750-7761
DOI: 10.1039/C5OB00962F, PaperMeriem K. Boukanoun, Xin Hou, Ljiljana Nikolajev, Sara Ratni, David Olson, Audrey Claing, Stephane A. Laporte, Sylvain Chemtob, William D. Lubell
The bioactive turn geometry of prostaglandin F2[small alpha] receptor modulators was investigated in pursuit of molecules that delay labor.
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A practical deca-gram scale ring expansion of (R)-(-)-carvone to (R)-(+)-3-methyl-6-isopropenyl-cyclohept-3-enone-1

16 July, 2015 - 02:54

Org. Biomol. Chem., 2015, 13,7633-7642
DOI: 10.1039/C5OB00525F, PaperLeandro de C. Alves, Andre L. Desidera, Kleber T. de Oliveira, Sean Newton, Steven V. Ley, Timothy J. Brocksom
A route to enantiopure (R)-(+)-3-methyl-6-isopropenyl-cyclohept-3-enone-1, an intermediate for terpenoids, has been developed and includes a highly chemo- and regioselective Tiffeneau-Demjanov reaction.
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A model [small beta]-sheet interaction and thermodynamic analysis of [small beta]-strand mimetics

12 July, 2015 - 02:17

Org. Biomol. Chem., 2015, 13,7402-7407
DOI: 10.1039/C5OB00886G, CommunicationColin W. Robinson, Carl S. Rye, Nicola E. A. Chessum, Keith Jones
Two novel [small beta]-strand mimetics are synthesized and their binding to a model peptide is studied in detail by 1H NMR.
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Copper(II)-promoted direct conversion of methylarenes into aromatic oximes

12 July, 2015 - 02:17

Org. Biomol. Chem., 2015, 13,7397-7401
DOI: 10.1039/C5OB00923E, CommunicationJiatao Yu, Ming Lu
A simple and efficient catalytic system for direct conversion of methylarenes into aromatic oximes has been developed, with Cu(OAc)2 as catalyst, NHPI (N-hydroxyphthalimide) as additive, tert-butyl nitrite (TBN) as both the nitrogen source and the oxidant. The process proceeds under mild conditions, tolerates a wide range of substrates, affording the corresponding aromatic oximes in 63-86% yields.
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Nickel-catalyzed Suzuki-Miyaura type cross-coupling reactions of (2,2-difluorovinyl)benzene derivatives with arylboronic acids

10 July, 2015 - 01:54

Org. Biomol. Chem., 2015, 13,7389-7392
DOI: 10.1039/C5OB01016K, CommunicationYang Xiong, Tao Huang, Xinfei Ji, Jingjing Wu, Song Cao
An unprecedented highly stereoselective example of nickel-catalyzed Suzuki-Miyaura type cross-coupling reactions of (2,2-difluorovinyl)benzene derivatives with arylboronic acids was developed.
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Synthesis of 2-deoxy-2,2-difluoro-[small alpha]-maltosyl fluoride and its X-ray structure in complex with Streptomyces coelicolor GlgEI-V279S

10 July, 2015 - 01:54

Org. Biomol. Chem., 2015, 13,7542-7550
DOI: 10.1039/C5OB00867K, PaperSandeep Thanna, Jared J. Lindenberger, Vishwanath V. Gaitonde, Donald R. Ronning, Steven J. Sucheck
Mycobacterium tuberculosis (Mtb) GlgE is a genetically validated TB drug target involved in [small alpha]-glucan biosynthesis. The Streptomyces coelicolor (Sco) GlgEI-V279S variant described here is used as a model enzyme for structure-based inhibitor design.
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Design, synthesis and biological evaluation of novel dimeric and tetrameric cRGD-paclitaxel conjugates for integrin-assisted drug delivery

10 July, 2015 - 01:54

Org. Biomol. Chem., 2015, 13,7530-7541
DOI: 10.1039/C5OB00497G, PaperA. Bianchi, D. Arosio, P. Perego, M. De Cesare, N. Carenini, N. Zaffaroni, M. De Matteo, L. Manzoni
Novel RGD-PTX multivalent conjugates, presenting enhanced binding for an [small alpha]v[small beta]3 integrin, have been reported. In vivo evaluation of 3b showed tumor growth inhibition through administering one-third of the PTX dose.
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Exploring carbonic anhydrase inhibition with multimeric coumarins displayed on a fullerene scaffold

10 July, 2015 - 01:54

Org. Biomol. Chem., 2015, 13,7445-7451
DOI: 10.1039/C5OB01005E, PaperMarta Abellan-Flos, Muhammet Tanc, Claudiu T. Supuran, Stephane P. Vincent
This study reports the first synthesis of multimeric suicide inhibitors of carbonic anhydrases.
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Expanding the scope of N [rightward arrow] S acyl transfer in native peptide sequences

10 July, 2015 - 01:54

Org. Biomol. Chem., 2015, 13,7469-7476
DOI: 10.1039/C5OB01029B, PaperBen Cowper, Leila Shariff, Wenjie Chen, Samantha M. Gibson, Wei-Li Di, Derek Macmillan
A wider variety of Xaa-Cys motifs than originally envisaged were capable of undergoing efficient N [rightward arrow] S acyl transfer to form thioesters and cyclic peptides, and our findings are applied to synthesis of wild-type Sunflower Trypsin Inhibitor-1 (SFTI-1).
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Enantioselective alkynylation of benzo[e][1,2,3]-oxathiazine 2,2-dioxides catalysed by (R)-VAPOL-Zn complexes: synthesis of chiral propargylic cyclic sulfamidates

10 July, 2015 - 01:54

Org. Biomol. Chem., 2015, 13,7393-7396
DOI: 10.1039/C5OB01012H, CommunicationLode De Munck, Alicia Monleon, Carlos Vila, M. Carmen Munoz, Jose R. Pedro
An enantioselective alkynylation of cyclic benzoxathiazine 2,2-dioxides catalysed by (R)-VAPOL-Zn(II) complexes is described.
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Twisted amide electrophiles enable cyclic peptide sequencing

8 July, 2015 - 01:17

Org. Biomol. Chem., 2015, 13,7384-7388
DOI: 10.1039/C5OB01050K, CommunicationSerge Zaretsky, Vishal Rai, Gerald Gish, Matthew W. Forbes, Michael Kofler, Joy C. Y. Yu, Joanne Tan, Jennifer L. Hickey, Tony Pawson, Andrei K. Yudin
Preserving the electrophilic carbonyl group of an aziridine amide in a macrocycle enables cyclic peptide sequencing by chemoselective linearization and tandem mass spectrometry.
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Tryptophan prenyltransferases showing higher catalytic activities for Friedel-Crafts alkylation of o- and m-tyrosines than tyrosine prenyltransferases

8 July, 2015 - 01:17

Org. Biomol. Chem., 2015, 13,7551-7557
DOI: 10.1039/C5OB01040C, PaperAili Fan, Xiulan Xie, Shu-Ming Li
Better conversion of L-o- and L-m-tyrosine to their C-prenylated derivatives by tryptophan prenyltransferases (Trp-PTs) than tyrosine O-prenyltransferases (Tyr-O-PT).
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Theoretical investigations of the reaction between 1,4-dithiane-2,5-diol and azomethine imines: mechanisms and diastereoselectivity

8 July, 2015 - 01:17

Org. Biomol. Chem., 2015, 13,7558-7569
DOI: 10.1039/C5OB00807G, PaperLinjie Zheng, Yan Qiao, Mengxue Lu, Junbiao Chang
The detailed mechanism of the DABCO-catalyzed reaction between 1,4-dithiane-2,5-diol and azomethine imines.
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Fluorinated enol ethers: their synthesis and reactivity

8 July, 2015 - 01:17

Org. Biomol. Chem., 2015, 13,7351-7380
DOI: 10.1039/C5OB00855G, Review ArticleM. Decostanzi, J.-M. Campagne, E. Leclerc
This review sums up the methods for the preparation of fluorinated enol ethers as well as their numerous synthetic applications.
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Synthesis and evaluation of a novel Rhodamine B pyrene [2]rotaxane as an intracellular delivery agent for doxorubicin

8 July, 2015 - 01:17

Org. Biomol. Chem., 2015, 13,7517-7529
DOI: 10.1039/C5OB00934K, PaperJiaxin Shi, Yuan Xu, Xinlong Wang, Luyong Zhang, Jing Zhu, Tao Pang, Xiaofeng Bao
RhBPy [2]rotaxane has been demonstrated to be an efficient transport agent for delivering the cancer drug doxorubicin (DOX) into tumor cells.
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Evaluation of the antibacterial and antibiofilm activities of novel CRAMP-vancomycin conjugates with diverse linkers

8 July, 2015 - 01:17

Org. Biomol. Chem., 2015, 13,7477-7486
DOI: 10.1039/C5OB00830A, PaperNigam M. Mishra, Yves Briers, Chris Lamberigts, Hans Steenackers, Stijn Robijns, Bart Landuyt, Jos Vanderleyden, Liliane Schoofs, Rob Lavigne, Walter Luyten, Erik V. Van der Eycken
Conjugates of CRAMP (cathelicidin-related antimicrobial peptides) and vancomycin were synthesised using click chemistry with diverse hydrophilic and hydrophobic linkers.
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Synthesis of benzimidazoles via iridium-catalyzed acceptorless dehydrogenative coupling

8 July, 2015 - 01:17

Org. Biomol. Chem., 2015, 13,7381-7383
DOI: 10.1039/C5OB00904A, CommunicationXiang Sun, Xiao-Hui Lv, Lin-Miao Ye, Yu Hu, Yan-Yan Chen, Xue-Jing Zhang, Ming Yan
Benzimidazoles were prepared in good yields via the iridium-catalyzed acceptorless dehydrogenative coupling of tertiary amines and arylamines.
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Interaction of myo-inositol hexakisphosphate with biogenic and synthetic polyamines

8 July, 2015 - 01:17

Org. Biomol. Chem., 2015, 13,7500-7512
DOI: 10.1039/C5OB00900F, PaperJulia Torres, Claudia Giorgi, Nicolas Veiga, Carlos Kremer, Antonio Bianchi
myo-Inositol hexakisphosphate (phytate) forms very stable adducts with biogenic and synthetic polyamines in aqueous solution.
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