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Half-sandwich (η5-Cp*)Rh(III) complexes of pyrazolated organo-sulfur/selenium/tellurium ligands: efficient catalysts for base/solvent free C–N coupling of chloroarenes under aerobic conditions

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00538J, Paper
Charu Sharma, Avinash Kumar Srivastava, Kamal Nayan Sharma, Raj Kumar Joshi
Three new Rh(III) complexes of organochalcogen (S/Se/Te) ligands were synthesized and along with a co-catalyst Cu(OAc)2, used for the base/solvent free catalysis of Buchwald type C–N coupling of amines and aryl chlorides under aerobic conditions.
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Photocatalytic xanthate-based radical addition/cyclization reaction sequence toward 2-biphenyl isocyanides: synthesis of 6-alkylated phenanthridines

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00136H, Communication
Pedro López-Mendoza, Luis D. Miranda
A photocatalytic xanthate-based radical addition/cyclization reaction cascade toward 2-biphenylisocyanides is described as a practical and modular approach to 6-alkylated phenanthridines.
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Electrochemical synthesis of selenyl-dihydrofurans via anodic selenofunctionalization of allyl-naphthol/phenol derivatives and their anti-Alzheimer activity

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00629G, Communication
Marcos R. Scheide, Alex R. Schneider, Guilherme A. M. Jardim, Guilherme M. Martins, Daniele C. Durigon, Sumbal Saba, Jamal Rafique, Antonio L. Braga
Herein, we report an eco-friendly, electrosynthetic approach for the intramolecular oxyselenylation of allyl-naphthol/phenol derivatives.
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Ni(II)-Catalyzed vinylic C–H functionalization of 2-acetamido-3-arylacrylates to access isotetronic acids

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00557F, Paper
Biswajit Roy, Eshani Das, Avijit Roy, Dipakranjan Mal
A ligand-free Ni(II)-catalyzed cascade annulation reaction for the synthesis of 4-aryl-substituted isotetronic acids from 2-acetamido-3-arylacrylates via vinylic C–H functionalization is reported.
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Asymmetric trehalose analogues to probe disaccharide processing pathways in mycobacteria

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00253D, Paper
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Hadyn L. Parker, Ruben M. F. Tomás, Christopher M. Furze, Collette S. Guy, Elizabeth Fullam
Chemoenzymatic synthesis of azido-functionalised asymmetric trehalose analogues that are resistant to enzymatic degradation to probe carbohydrate processing pathways in mycobacteria.
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Heterologous expression of the trichostatin gene cluster and functional characterization of N-methyltransferase TsnB8

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00617C, Communication
Wei Liu, Vinay Gopal Jannu, Zhiwen Liu, Qingbo Zhang, Xiaodong Jiang, Liang Ma, Wenjun Zhang, Changsheng Zhang, Yiguang Zhu
N-Methyltransferase TsnB8 was demonstrated to catalyze successive methyltransfer reactions in the biosynthesis of trichostatin.
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Donor–acceptor fluorophores as efficient energy transfer photocatalysts for [2 + 2] photodimerization

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/C9OB02735A, Paper
Qing-An Wu, Feng Chen, Chen-Chao Ren, Xue-Fen Liu, Hao Chen, Liang-Xuan Xu, Xiao-Cong Yu, Shu-Ping Luo
Donor–acceptor fluorophores can act as efficient energy transfer photocatalysts to activate enone substrates, realizing photodimerization and isomerization reaction of enone substrates without precious metal photocatalysts.
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Catalyst- and Solvent-Free Efficient Access to N-Alkylated Amines via Reductive Amination using HBPin

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00740D, Communication
ARNAB RIT, Vipin Kumar Pandey, Somnath Bauri
A sustainable approach which works under catalyst- and solvent-free conditions for the synthesis of structurally diverse secondary amines has been uncovered. This one-pot protocol works efficiently at room temperature and...
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A laccase-catalysed tyrosine click reaction

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00650E, Communication
Shinichi Sato, Keita Nakane, Hiroyuki Nakamura
The tyrosine click reaction of peptides/proteins with the tyrosine modification reagent, N-methyl luminol, was catalysed by a laccase in the presence of molecular oxygen (O2) at 37 °C.
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A silver-catalyzed radical ring-opening reaction of cyclopropanols with sulfonyl oxime ethers

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00055H, Paper
Xiaobao Zeng, Xin Wang, Yanan Zhang, Li Zhu, Yu Zhao
A simple and efficient method for the radical ring-opening reaction of cyclopropanols with sulfonyl oxime ethers catalyzed by AgNO3 is developed, affording γ-keto oxime ethers in moderate to good yields.
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Discrimination of cellular developmental states focusing on glycan transformation and membrane dynamics by using BODIPY-tagged lactosyl ceramides

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00547A, Paper
Kenta Arai, Atsuko Ohtake, Shusaku Daikoku, Katsuhiko Suzuki, Yukishige Ito, Kazuya Kabayama, Koichi Fukase, Yoshimi Kanie, Osamu Kanie
Different cellular states were discriminated by analysing either the glycan transformation of exogenously introduced fluorescently tagged probe molecules or fluorescence recovery after photobleaching before conversion.
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Electrochemically enabled functionalization of indoles or anilines to synthesis of hexafluoroisopropoxy indole and anilinederivatives

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00157K, Communication
Zu-yu Mo, Xin-Yu Wang, Yu-zhen Zhang, Li Yang, Hai-Tao Tang, Ying-Ming Pan
An environmentally benign electrochemically enabled site-selective functionalization of indole or aniline derivatives with hexafluoroisopropanol in the presence of tetrabutyl ammonium hexafluorophosphate as redox catalyst and electrolyte was demonstrated in this...
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Synthesis of unsymmetrical benzils via palladium-catalysed α-arylation–oxidation of 2-hydroxyacetophenones with aryl bromides

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00575D, Paper
Open Access
Takanori Matsuda, Souta Oyama
Unsymmetrical benzils are synthesised by a one-pot tandem palladium-catalysed α-arylation and oxidation of 2-hydroxyacetophenones with aryl bromides.
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Enantioselective Synthesis of Indanone Spiro-Isochromanone Derivatives via Dinuclear Zinc-Catalyzed Michael/Transesterification Tandem Reaction

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00541J, Paper
Xiao-Chao Yang, Meng Xu, Jin-Bao Wang, Meng-Meng Liu, Francois Mathey, Yuan-Zhao Hua, Mincan Wang
An enantioselective Michael/transesterification tandem reaction of α-hydroxy indanones with ortho-ester chalcones was realized by dinuclear zinc catalysts. A series of enantiomerically pure spiro[indanone-2,3’-isochromane-1-one] derivatives were obtained in good yields with...
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Synthesis and photophysical properties of selenopheno[2,3-b]quinoxaline and selenopheno[2,3-b]pyrazine heteroacenes

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00718H, Paper
Amol Sonawane, Atsushi Shimozuma, Taro Udagawa, Masayuki Ninomiya, Mamoru Koketsu
In this paper, we report the novel synthesis of three different heterocycles namely 2-arylselenopheno[2,3-b]quinoxaline, 3-(aryl/alkylselanyl)-2-arylselenopheno[2,3-b]quinoxaline and 6-phenyl-7-(arylselanyl)selenopheno[2,3-b]pyrazine derivatives from the corresponding 2,3-dichloroquinoxaline and 2,3-dichloropyrazine derivatives. Further, photophysical properties were investigated...
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Protein labeling approach to improve lysosomal targeting and efficacy of antibody–drug conjugates

Org. Biomol. Chem., 2020, 18,3229-3233
DOI: 10.1039/D0OB00265H, Communication
Ying Han, Yifan Da, Mingjia Yu, Yaping Cheng, Xin Wang, Jiale Xiong, Guoying Guo, Yan Li, Xianxing Jiang, Xiaoqing Cai
An anti-EGFR nanobody was labeled at the C-terminus with a lysosome-sorting NPGY (Asn-Pro-Gly-Tyr) motif via sortase-mediated ligation to enhance the clathrin-mediated endocytosis.
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Targeting STAT3 anti-apoptosis pathways with organic and hybrid organic–inorganic inhibitors

Org. Biomol. Chem., 2020, 18,3288-3296
DOI: 10.1039/C9OB02682G, Paper
Matthew B. Minus, Haopei Wang, Jaime O. Munoz, Alexandra M. Stevens, Alicia E. Mangubat-Medina, Michael J. Krueger, Wei Liu, Moses M. Kasembeli, Julian C. Cooper, Mikhail I. Kolosov, David J. Tweardy, Michele S. Redell, Zachary T. Ball
Recurrence and drug resistance are major challenges in the treatment of acute myeloid leukemia (AML) that spur efforts to identify new clinical targets and active agents.
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Synthesis, structures and photophysical properties of hexacoordinated organosilicon compounds with 2-(2-pyridyl)phenyl groups

Org. Biomol. Chem., 2020, 18,3239-3242
DOI: 10.1039/D0OB00484G, Communication
Shohei Furuta, Toshiaki Mori, Yusuke Yoshigoe, Kohei Sekine, Yoichiro Kuninobu
We synthesised novel air-, water-, heat-, acid-, and base-stable hexacoordinated organosilicon compounds, which contain two C,N-bidentate ligands and form two silafluorene equivalent moieties, with Lewis acid–base interactions.
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Synthetic pathways to tetrahydrocannabinol (THC): an overview

Org. Biomol. Chem., 2020, 18,3203-3215
DOI: 10.1039/D0OB00464B, Review Article
Open Access
Victor R. L. J. Bloemendal, Jan C. M. van Hest, Floris P. J. T. Rutjes
This review summarises various synthetic pathways leading to tetrahydrocannabinol and structurally related cannabinoids.
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Three-component synthesis of 1,4-benzothiazines via iodide-catalyzed aerobic C–H sulfuration with elemental sulfur

Org. Biomol. Chem., 2020, 18,3234-3238
DOI: 10.1039/D0OB00074D, Communication
Jingjing Jiang, Xiaolong Tuo, Zhuquan Fu, Huawen Huang, Guo-Jun Deng
Five to Six: Beyond the well-established thiazole formation from elemental sulfur, this method provides the first access to the corresponding six-membered N,S-heterocyclic products via direct functionalization of multiple C–H bonds.
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Phenylboronic acid-catalyzed tandem construction of S–S and C–S bonds: a new method for the synthesis of benzyl disulfanylsulfone derivatives from S-benzyl thiosulfonates

Org. Biomol. Chem., 2020, 18,3243-3248
DOI: 10.1039/D0OB00442A, Communication
Raju Jannapu Reddy, Md. Waheed, Gamidi Rama Krishna
A novel and unique phenylboronic acid-catalyzed tandem construction of S–S and C–S bonds via dimerization–sulfonylation has been disclosed for the synthesis of benzyl disulfanylsulfone derivatives.
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Visible light induced 3-position-selective addition of arylpropiolic acids with ethers via C(sp3)–H functionalization

Org. Biomol. Chem., 2020, 18,3258-3262
DOI: 10.1039/D0OB00480D, Communication
Zi-juan Wan, Xiao-feng Yuan, Jun Luo
Although the 2-position-selective decarboxylative coupling or addition of arylpropiolic acids with cyclic ethers has been intensively investigated, selective functionalization of arylpropiolic acids at the 3-position is still a big challenge.
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Copper-catalyzed direct amination of benzylic hydrocarbons and inactive aliphatic alkanes with arylamines

Org. Biomol. Chem., 2020, 18,3263-3268
DOI: 10.1039/D0OB00491J, Communication
Hua Yao, Bo Xie, Xiaoyang Zhong, Shengzhou Jin, Sen Lin, Zhaohua Yan
A new synthetic method toward direct C–N bond formation through saturated C–H amination of benzylic hydrocarbons and inactive aliphatic alkanes with primary aromatic amines under an inexpensive catalyst/oxidant (Cu/DTBP) system has been developed.
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A base-promoted tandem approach to bicyclic 8-membered ring ketones

Org. Biomol. Chem., 2020, 18,3249-3253
DOI: 10.1039/D0OB00618A, Communication
Emerson E. F. dos Santos, Gabriela F. P. de Souza, Deborah A. Simoni, Airton G. Salles
A base-promoted tandem route toward unprecedented bicyclic furan/8-membered ring ketones is reported.
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Chemo- and regioselective click reactions through nickel-catalyzed azide–alkyne cycloaddition

Org. Biomol. Chem., 2020, 18,3374-3381
DOI: 10.1039/D0OB00579G, Paper
Woo Gyum Kim, Seung-yeol Baek, Seo Yeong Jeong, Dongsik Nam, Ji Hwan Jeon, Wonyoung Choe, Mu-Hyun Baik, Sung You Hong
Nickel-catalyzed [3 + 2] cycloaddition reactions of unsymmetrical alkynes and organic azides afford substituted 1,2,3-triazoles with high levels of chemo- and regioselectivity.
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Chiral bifunctional sulfide-catalyzed asymmetric bromoaminocyclizations

Org. Biomol. Chem., 2020, 18,3367-3373
DOI: 10.1039/D0OB00459F, Paper
Takumi Nakamura, Ken Okuno, Kazuma Kaneko, Masahiro Yamanaka, Seiji Shirakawa
A chiral bifunctional sulfide catalyst bearing a urea moiety promotes the enantioselective bromoaminocyclization of 2-allylanilines to produce optically active 2-substituted indolines.
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Dipyrazolodioxadiazocines as shelf-stable “ready-to-use” precursors for an in situ generation of enolate-iminium 1,4-dipoles: a straightforward atom-economical approach to pyrazolo[5,1-d][1,3,5]dioxazines

Org. Biomol. Chem., 2020, 18,3382-3391
DOI: 10.1039/D0OB00451K, Paper
Vladimir E. Zhulanov, Valeria A. Vigovskaya, Maksim V. Dmitriev, Pavel S. Silaichev, Andrey N. Maslivets, Michael Rubin
Generation of cyclic enolate-iminium 1,4-dipoles via thermolysis of dipyrazolodioxadiazocines in the presence of ketones allowed for efficient preparation of pyrazolo[5,1-d][1,3,5]dioxazines.
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Correction: Synthetic-biology-based discovery of a fungal macrolide from Macrophomina phaseolina

Org. Biomol. Chem., 2020, 18,3392-3392
DOI: 10.1039/D0OB90051F, Correction
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Yohei Morishita, Terutaka Sonohara, Tohru Taniguchi, Kiyohiro Adachi, Makoto Fujita, Teigo Asai
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Controlling the liberation rate of the in situ release of a chemical fuel for the operationally autonomous motions of molecular machines

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00669F, Paper
Chiara Biagini, Giorgio Capocasa, Daniele Del Giudice, Valerio Cataldi, Luigi Mandolini, Stefano Di Stefano
Aminolysis of the anhydride of 2-cyano-2-phenylpropanoic acid can be employed to conveniently regulate the liberation rate of the related acid which, in turn, can be used as a fuel for acid–base operated molecular machines.
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Late-stage synthesis and application of photoreactive probes derived from direct benzoylation of heteroaromatic C–H bonds

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00336K, Communication
Kevin D. Hesp, Jun Xiao, Graham M. West
A synthetically-driven, late-stage C–H benzoylation strategy for the expedited preparation and evaluation of heterocyclic alternatives to more classical benzophenone photoreactive probes is reported.
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Dienaminodioate based multicomponent reactions with post-benzylic oxidative transformations mediated by DDQ

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00721H, Paper
Jaice Ravindran, Velickakathu Yadhukrishnan, Reghuvaran Asha , Ravi Shankar Lankalapalli
Multicomponent reactions (MCRs) using dienaminodioate with post-benzylic oxidative transformation by DDQ that afforded a diverse array of products is described. An unprecedented rearrangement of 1,2-dihydropyridines (1,2-DHPs), 3CR products, to 2-pyridones...
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Spiroconyone A, a new phytosterol with a spiro [5,6] ring system from Conyza japonica

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00666A, Paper
Long-Gao Xiao, Yu Zhang, Hong-Li Zhang, Ding Li, Qiong Gu, Gui-Hua Tang, Qian Yu, Lin-Kun An
The first rearranged phytosterol (spiroconyone A) with an unusual spiro [5,6] ring system and two new TDP1 inhibitors 7 and 10 showing a strong synergistic effect with topotecan were isolated from Conyza japonica.
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Synthesis of gem-difluoroalkenes via nickel-catalyzed allylic defluorinative reductive cross-coupling of trifluoromethyl alkenes with epoxides

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB00535E, Communication
Xiao-Yu Lu, Run-Chuang Jiang, Jia-Mei Li, Chuang-Chuang Liu, Qing-Qing Wang, Hai-Pin Zhou
A nickel-catalyzed defluorinative reductive cross-coupling of trifluoromethyl alkenes with epoxides has been developed.
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Arylation of Indoles Using Cyclohexanones Dually-Catalyzed by Niobic Acid and Palladium-on-Carbons

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00702A, Paper
Kazuho Ban, Yuta Yamamoto, Hironao Sajiki, Yoshinari Sawama
3-Arylindoles were easily constructed from indoles and cyclohexanone derivatives using a combination of catalytic niobic acid-on-carbon (Nb2O5/C) and palladium-on-carbon (Pd/C) under heating conditions without any oxidants. The Lewis acidic Nb2O5/C...
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Hierarchical Self-Assembly of Azobenzene Dyad with Inverted Amide Connection into Toroidal and Tubular Nanostructures

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00833H, Communication
Shiki Yagai, Takuho Saito
Inversion of the connectivity of amide groups in foldable azobenzene dyads with chiral side chains, which can self-assemble into toroids and nanotubes, significantly increases the thermal stability of these aggregates....
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Correction: Nickel-catalyzed cyanation of phenol derivatives activated by 2,4,6-trichloro-1,3,5-triazine

Org. Biomol. Chem., 2020, Advance Article
DOI: 10.1039/D0OB90052D, Correction
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Liang Wang, Yaoyao Wang, Jun Shen, Qun Chen, Ming-Yang He
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Efficient synthesis of a galectin inhibitor clinical candidate (TD139) using a Payne rearrangement/azidation reaction cascade

Org. Biomol. Chem., 2020, Accepted Manuscript
DOI: 10.1039/D0OB00910E, Paper
Jacob St-Gelais, Vincent Denavit, Denis Giguère
Selective galectin inhibitors are valuable research tools and could also be used as drug candidates. In that context, TD139, a thiodigalactoside galectin-3 inhibitor, is currently being evaluated clinically for the...
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Fire arm, opening an eatery: get licence application forms online

Now, getting a licence for a fire-arm or operating an eatery will be easy with Delhi Police on Tuesday launching a dedicated website for its Licencing Branch.




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Cos use foreign money for political funding. Isn’t that influencing polls?

A recent Intelligence Bureau (IB) report has claimed that some well-known NGOs are working to stall economic development at the behest of their foreign donors. Activists and rights groups have been up in arms ever since the report was leaked.




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Pak politicians want to resolve Kashmir — military won't allow this: Arif Jamal

Arif Jamal is a Pakistani journalist and South Asia expert based in America.




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​'Advertising's art of persuasion — political ads will grow': Prasoon Joshi

Author and advertising authority headed the Titanium Lions jury at 2014's Cannes International Advertising Festival.




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There’s no power politics, customer is king, Piyush Goyal says

The responsibility of lighting up the country today rests on Piyush Goyal’s shoulders. Just a month into his new job, the minister for power, coal and renewable energy has set an electric pace to energize the sector.




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Australia-India cricket rivalry has even bettered Ashes: John Harnden

CEO of the ICC World Cup 2015 John Harnden spoke with Amin Ali about ensuring excitement in cricket's mega-tournament, clamping down on racism, managing 'minnows' matches — and how Australia is sizing up India as a rival for the trophy.




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Officials to pay for illegal building: Venkaiah Naidu

The Centre will push for key reforms including the provision of incentivising civic agencies for good work & making officials concerned accountable for illegal construction or unauthorized development under their jurisdiction.




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Indian American Christians condemn assassination of Bhatti

Strongly condemning the assassination of Shahbaz Bhatti, the Federation of Indian Christians Organisations of North America appealed to Islamabad to bring the perpetrators of the "dastardly" crime to justice.




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Hindu guru convicted of molesting girls in US

An octogenarian Hindu religious leader, head of a Hindu ashram, one of the largest temples in the US, has been convicted of molesting two young girls.




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Indian-American scientists develop alternative to radio tags

A team of Indian-American scientists has developed a smart tracking system, which could very well provide an honourable alternative to the radio tags.




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S African-Indian women get 3-yr jail for fraud

An Indian-origin woman and her mother were sentenced to three years in prison by a South African court, which found them guilty of arranging a fake certificate of marriage to inherit property of their landlord, who died of poisoning.




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Australia's Victoria police inducts first turban wearing Sikh

Police in Australia's Victoria state today inducted its first officer from Sikh community who will wear a newly designed police turban, a media report said today.




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Gujarati icing on Will-Kat wedding cake!

The royal wedding cake is set to have a Gujarati connection. It has emerged that Prince William and Kate Middleton have chosen a cake company run by a Gujarati in Leicestershire.