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Lead optimisation of OXS007417: in vivo PK profile and hERG liability modulation to optimise a small molecule differentiation agent for the potential treatment of acute myeloid leukaemia

RSC Med. Chem., 2024, 15,3495-3506
DOI: 10.1039/D4MD00275J, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Thomas J. Cogswell, Laia Josa-Culleré, David Zimmer, Sébastien R. G. Galan, Morgan Jay-Smith, Kate S. Harris, Carole J. R. Bataille, Thomas R. Jackson, Douzi Zhang, Stephen G. Davies, Paresh Vyas, Thomas A. Milne, Graham M. Wynne, Angela J. Russell
The optimisation of a class of AML differentiation agents is described to show improved potency, solubility and stability, reduced off target toxicity, and tumour regression in a murine model in vivo.
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Discovery of highly potent SARS-CoV-2 nsp14 methyltransferase inhibitors based on adenosine 5'-carboxamides

RSC Med. Chem., 2024, 15,3469-3476
DOI: 10.1039/D4MD00422A, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Hugo Kocek, Dominika Chalupská, Milan Dejmek, Alexandra Dvořáková, Michala Zgarbová, Michal Šála, Karel Chalupský, Petra Krafčíková, Tomáš Otava, Matúš Drexler, Eliška Procházková, Blanka Klepetářová, Milan Štefek, Ján Kozic, Helena Mertlíková-Kaiserová, Evzen Boura, Jan Weber, Radim Nencka
SARS-CoV-2 nsp14 methyltransferase inhibitors based on adenosine 5'-carboxamides.
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Design, synthesis and mechanistic insights into triclosan derived dimers as potential anti-plasmodials

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00494A, Research Article
Shekhar, Shefali Chowdhary, Joel Mosnier, Isabelle Fonta, Bruno Pradines, Vipan Kumar
In pursuit of novel anti-plasmodial agents, a library of triclosan-based dimers both with and without a 1H-1,2,3 triazole core were designed, synthesized and evaluated in order to achieve a multitargeted approach.
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Continuous flow synthesis of N,N-dimethyltryptamine (DMT) analogues with therapeutic potential

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00562G, Research Article
Open Access
Andreas Simoens, Andreas Dejaegere, Marthe Vandevelde, Christian V. Stevens
Flow chemistry allows for the rapid and clean synthesis of therapeutically relevant tryptamines in good yields, including the large scale drug rizatriptan.
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Ligand-centred phenotype-driven development of potent kinase inhibitors against oesophageal cancer

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00579A, Research Article
Open Access
Cecilia C. Ayala-Aguilera, Yang Ge, Álvaro Lorente-Macías, Benjamin N. Jones, Catherine Adam, Neil O. Carragher, Asier Unciti-Broceta
A ligand-centred strategy combined with phenotypic screening was used to develop novel antiproliferative inhibitors against oesophageal cancer and identified a lead compound that induces potent anticancer activity and inhibits Aurora kinase A.
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Synthesis and anti-tumor activity of new benzofuran-based chalcone derivatives as potent VEGFR-2 inhibitors

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00621F, Research Article
Chunfei Zhang, Yixin Liu, Xiao Zhang, Chunping Wan, Zewei Mao
A series of novel benzofuran-based chalcone derivatives could be considered as potent VEGFR-2 inhibitors.
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S-MGBs bearing amidine tail groups are potent, selective antiplasmodial agents

RSC Med. Chem., 2024, Advance Article
DOI: 10.1039/D4MD00619D, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Marina Perieteanu, Tayner Rodriguez Garzon, Leah M. C. McGee, Abedawn I. Khalaf, Colin J. Suckling, Rebecca Beveridge, Vicky M. Avery, Fraser J. Scott
25 S-MGBs, including those bearing an amidine tail group, were investigated for their antiplasmodial, in vitro activity against 3D7 and Dd2 strains of P. falciparum. Several potent, and selective, hit compounds were identified.
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Design and synthesis of (E)-3-benzylideneindolin-2-one derivatives as potential allosteric inhibitors of Aurora A kinase

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00373J, Research Article
YongLai Jiao, Jie Zhong, Jin-Fang Xu, Shaobo Ning, Taigang Liang, Mingzhu Zhao, Jian Zhang
The mitotic kinase Aurora A, a pivotal regulator of cell cycle, is overexpressed in various cancers and has emerged as one of the most promising targets for anticancer drug discovery....
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pot

Investing in companies with ‘indicorn’ potential

Titan Capital backs seed-stage companies with potential to reach ₹100 crore revenue within five years




pot

Brand expertise and heritage bubbling in a moka pot

Lessons from European brands that have won consumers’ mindspace for long years




pot

Spotlight on ways to end violence against children




pot

IIT Delhi’s annual Open House shows AI’s potential use in health care, tech




pot

M.S. Swaminathan, the scientist who sliced potatoes

Not once did the ‘Rice Man of India’ keep his publisher waiting




pot

After snails, farmers in Idukki battling spotted locust infestation; experts say change in climate pattern could be a cause

Plantations of over 70 farmers severely affected by the spotted locust infestation at Konnathady and Vathikudy panchayats




pot

‘India is a bright spot in global smartphone scene’




pot

The cellular Potts model on disordered lattices

Soft Matter, 2024, 20,8337-8352
DOI: 10.1039/D4SM00445K, Paper
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Hossein Nemati, J. de Graaf
Extending the cellular Potts model to disordered Voronoi lattices reduces artifacts observed on regular lattices. An order–disorder transition is observed as a function of surface tension on the disordered lattice and the regular lattices.
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Celebspotting: Lakme Fashion Week Winter/Festive 2016

Who modelled for whom during this year's edition of Lakme Fashion Week's Winter collection?




pot

Editorial. Biden’s late withdrawal leaves the Democrats in a spot

The Democrats now have to decide afresh a new candidate to replace Biden and, as a result, their overall response to Trump whose worldview is diametrically the opposite to theirs




pot

‘Karthika Masa Laksha Deepotsavam’ concludes on a grand note in Nellore

501 couples participate in the ‘Veera Venkata Satyanarayana Swamy Vratam’ organised on the occasion




pot

Good potential for cosmetic, textile, food processing sectors in Andhra Pradesh: South Korean diplomat

South Koreans are familiar with Andhra Pradesh and since Kia Motors is here, more Korean companies may wish to come too, says Sangwoo Lim




pot

Spotlighting the work of the Economics Nobel winners

AJR have emphasised the role of institutions in development but there has been criticism of this approach as privileging western liberal institutions




pot

Karnataka’s untapped tourism potential

The State has not capitalised on its rich cultural, religious, and natural heritage




pot

Address problems in accident black spots scientifically, Udupi DC tells officials




pot

As its industry struggles, Germany services sector offers untapped growth potential




pot

Veil spotting




pot

‘Panchathantram’ movie review: This anthology is a potpourri and the women make it watchable 

With Brahmanandam as a storyteller, the Telugu anthology film ‘Panchathantram’ looks at memories through sensory experiences and a couple of stories hit the sweet spot




pot

‘Anger Tales’ anthology review: Potpourri of hits and misses

The Telugu anthology ‘Anger Tales’ explores anger that stems from everyday situations through effective performances 




pot

Facile one-pot synthesis of novel imidates as multifunctional organic fluorescent materials

Org. Chem. Front., 2024, Advance Article
DOI: 10.1039/D4QO01628A, Research Article
Feng-Ting Liu, Shuo Wang, Yong-Shun Chen, Jun-Ying Miao, Bao-Xiang Zhao, Zhao-Min Lin
A novel one-pot synthesis of multifunctional organic fluorescent imidates from quinolinium salt derivatives, nitrosoarenes and alcohols was presented. This method had a wide substrate scope and excellent isolated yields.
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Synthesis of bambusurils with perfluoroalkylthiobenzyl groups as highly potent halide receptors

Org. Chem. Front., 2024, Advance Article
DOI: 10.1039/D4QO01746C, Research Article
Open Access
Matúš Chvojka, Hennie Valkenier, Vladimír Šindelář
Four new fluorinated bambusuril macrocycles were prepared to show exceptional high binding affinity towards halide anions in acetonitrile.
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DABSO-Mediated Pummerer Reaction Enables One-Pot Synthesis of Pyrroloquinolines for Accessing Marinoquinolines: Mechanistic, Photophysical and Pharmacological Investigations

Org. Chem. Front., 2024, Accepted Manuscript
DOI: 10.1039/D4QO01512F, Research Article
Rahimuddin Khan, Dipun Kumar Penthi, Aditi Chatterjee, Chandrakanta Sahoo, Shanti Gopal Patra, Viswanathan Arun Nagaraj, Tabrez Khan
A new one-pot acid- and exogenous oxidant-free synthesis of pyrrolo[2,3-c]quinolines has been developed. The strategy involves chemoselective reduction of the 3-(2-nitrophenyl)-1H-pyrroles (pyrrolnitrin derivatives) and subsequent DABSO-facilitated Pummerer reaction in the...
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World Test Championship standing: India loses top spot to Australia, slips to second

India lost to New Zealand by 25 runs in the third and final Test in Mumbai resutling in a 0-3 whitewash, their first in a home Test series since South Africa's 2-0 win in 1999-2000




pot

Carbonate weakens the interactions between potassium and calcareous soil

RSC Adv., 2024, 14,35275-35285
DOI: 10.1039/D4RA05988C, Paper
Open Access
Wei Du, Shifeng Wang, Yizhe Yang, Chenyang Xu, Feinan Hu, Wuquan Ding, Jialong Lv
Adsorption energies of K+ in carbonate-removed (CREM) and carbonate-reserved (CRES) calcareous soil.
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Synthesis and antibiotic potential of myxocoumarin-inspired chromene dione analogs

RSC Adv., 2024, 14,35215-35219
DOI: 10.1039/D4RA05941G, Paper
Open Access
Antonia Behnsen, Gesa Hertrampf, Sandra Vojnović, Jasmina Nikodinović-Runić, Tobias A. M. Gulder
The myxocoumarins are natural products with strong antibiotic activity. We herein explored structural simplification of the myxocoumarins while aiming to retain their antibacterial properties. This led to the discovery of potent myxochromene diones.
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Design, synthesis, and evaluation of novel thiadiazole derivatives as potent VEGFR-2 inhibitors: a comprehensive in vitro and in silico study

RSC Adv., 2024, 14,35505-35519
DOI: 10.1039/D4RA04158E, Paper
Open Access
Ibrahim H. Eissa, Walid E. Elgammal, Hazem A. Mahdy, Susi Zara, Simone Carradori, Dalal Z. Husein, Maymounah N. Alharthi, Ibrahim M. Ibrahim, Eslam B. Elkaeed, Hazem Elkady, Ahmed M. Metwaly
This study aims to investigate the potential of designed 2,3-dihydro-1,3,4-thiadiazole derivatives as anti-proliferative agents targeting VEGFR-2, utilizing a multidimensional approach combining in vitro and in silico analyses.
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Avinash Sable overwrites own meet record, Kushare consolidates Paris spot

The national record holder Avinash Sable, who has already attained the Paris Olympic qualifying standard, clocked 8:31.75 to overwrite his own previous meet record of 8:33.19, set five years ago in Lucknow.




pot

Silver futures rise on spot demand

Silver prices mainly rise due to fresh positions built up by participants on a positive domestic trend, say analysts



  • Gold & Silver

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Unravelling the potential of low-valent tunable vanadium complexes in the nitrogen reduction reaction (NRR)

Dalton Trans., 2024, Advance Article
DOI: 10.1039/D4DT02217C, Paper
Bijoy Ghosh, Sahtaz Ahmed, Ashwini K. Phukan
Comprehensive computational investigations predict the potential of several hitherto unknown tripodal vanadium complexes in the nitrogen reduction reaction (NRR) without the probability of generation of hydrazine as a side product.
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One-pot facile synthesis of rod-like Bi2S3 particles in deep eutectic solvent and their ppb-level selective H2S gas detection

Dalton Trans., 2024, Advance Article
DOI: 10.1039/D4DT03006K, Communication
Reiko Furukawa, Takuya Hasegawa, Ayahisa Okawa, Shu Yin
Rod-like Bi2S3 particles were synthesized by one-pot reactions with choline chloride-based DESs, and showed sub-ppm level selective H2S gas detection. Acetamide-based DES yielded uniform particles with excellent gas sensitivity.
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Improved microbial water quality and ozone performance following coagulation: implications for carbon based advanced treatment for potable reuse

Environ. Sci.: Water Res. Technol., 2024, Advance Article
DOI: 10.1039/D4EW00638K, Paper
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Christina M. Morrison, Ariel J. Atkinson, Daniel Gerrity, Eric C. Wert
Coagulation/flocculation of secondary effluent with FeCl3 (1) removed MS2 bacteriophage and bacterial endospores up to 2–3 LRVs, (2) removed rapid surrogates at levels correlative with microbial removal, and (3) improved downstream O3 performance.
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Is sugar in a sweet spot?

Prices will remain in the same range, between ₹3,600 and ₹3,700 per tonne, says Vijay S Banka




pot

IIMA proves it is gold standard for management studies, bags top spot in NIRF list for 5th consecutive time

Institute has been topping NIRF’s list of best management colleges since 2020




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An electric double layer regulator empowers robust solid-electrolyte interphase for potassium metal batteries

Energy Environ. Sci., 2024, Accepted Manuscript
DOI: 10.1039/D4EE03978E, Paper
Xueyu Lian, Liang Xu, Zhijing Ju, Ziang Chen, Xiaopeng Chen, Yuyang Yi, Zhengnan Tian, Tao Cheng, Shi Xue Dou, Xinyong Tao, Jingyu Sun
The electric double layer (EDL) plays a key role in constructing solid electrolyte interphase (SEI) for high-energy metal anodes. Nevertheless, the significance of EDL and its associated influence remain elusive...
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Stray dog menace puts Railways, Kozhikode Corporation in a spot

A tourist from Germany was bitten by a stray dog at the Kozhikode railway station recently




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Surface treatment of magnetite nanoparticle thin films with potassium phosphate for calcium phosphate precipitation

React. Chem. Eng., 2024, 9,782-786
DOI: 10.1039/D4RE00048J, Communication
Reo Kimura, Kazuto Sugimoto, Iori Yamada, Motohiro Tagaya
The treatment of magnetite nanoparticle thin films with potassium phosphate and their surface reaction with simulated body fluid were in situ monitored by the QCM-D technique, which is suitable for the precipitation of calcium phosphate.
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Spotted! Preity's husband at Wankhede

Bollywood actor Preity Zinta was spotted at the Wankhede stadium on Saturday afternoon with her husband Gene Goodenough.




pot

Spotted! Rishabh Pant's Lady Love

Isha will be hoping that Rishabh's luck changes for the better and DC makes the playoffs on the back of his batting and captaincy.




pot

Birthday Boy Dhoni Spotted At Wimbledon

Dhoni will be 41 on July 7.




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Pant Spotted At Dhoni's Birthday Party

On Wednesday night, Sakshi Singh Dhoni posted a video on Instagram of her husband bringing in his 41st birthday in London.




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Unravelling the potential of yolkin for nutraceutical use: the origin, structure, and functional insights of a hen egg yolk polypeptide complex

Food Funct., 2024, 15,10746-10760
DOI: 10.1039/D4FO03023K, Paper
Open Access
Aleksandra Zambrowicz, Katarzyna Kapczyńska, Paweł Kania, Jakub Stanisław Nowak, Marta Kaszowska, Katarzyna Szymczak-Kulus, Wioletta Kazana-Płuszka, Marta Piksa, Sabina Górska, Dominika Jakubczyk, Józefa Macała, Agnieszka Zabłocka
The nutraceutical potential of yolkin health benefits from hen egg yolk.
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Antigenotoxic and cosmetic potential of elderberry (Sambucus nigra) extract: protection against oxidative DNA damage

Food Funct., 2024, 15,10795-10810
DOI: 10.1039/D4FO03217A, Paper
Sara Gonçalves, Francisco Peixoto, Tayse F. F. da Silveria, Lillian Barros, Isabel Gaivão
The integrity of the genome is under constant threat from both endogenous and exogenous factors that induce oxidative stress and accelerate ageing.
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