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Discovery and optimisation of pyrazolo[1,5-a]pyrimidines as aryl hydrocarbon receptor antagonists

RSC Med. Chem., 2024, 15,3477-3484
DOI: 10.1039/D4MD00266K, Research Article
Raitis Bobrovs, Svetlana Terentjeva, Ninni Elise Olafsen, Zilvinas Dambrauskas, Antanas Gulbinas, Toivo Maimets, Indrek Teino, Aigars Jirgensons, Jason Matthews, Kristaps Jaudzems
The aryl hydrocarbon receptor (AHR) is a versatile ligand-dependent transcription factor involved in diverse biological processes, from metabolic adaptations to immune system regulation.
The content of this RSS Feed (c) The Royal Society of Chemistry




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Sidechain structure–activity relationships of cyclobutane-based small molecule αvβ3 antagonists

RSC Med. Chem., 2024, 15,3616-3624
DOI: 10.1039/D4MD00306C, Research Article
Open Access
  This article is licensed under a Creative Commons Attribution 3.0 Unported Licence.
Adam Throup, Manar Saleh Zraikat, Andrew Gordon, Shohreh Jafarinejad Soumehsaraei, Kathrin D. Haase, Laurence H. Patterson, Patricia A. Cooper, Katherine Hanlon, Paul M. Loadman, Mark Sutherland, Steven D. Shnyder, Helen M. Sheldrake
Cyclobutanes provide a versatile scaffold for the synthesis of small molecule integrin antagonists with good metabolic stability and in vivo tolerability.
The content of this RSS Feed (c) The Royal Society of Chemistry




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3-Thio-3,4,5-Trisubstituted-1,2,4-Triazoles: High Affinity Somatostatin Receptor-4 Agonist Synthesis and Structure-Activity Relationships

RSC Med. Chem., 2024, Accepted Manuscript
DOI: 10.1039/D4MD00597J, Research Article
Albert Michael Crider, Audrey Hospital, Karin Sandoval, William Neumann, Stephen Kukielski, Lejla Garic, Kristen Ingold, Matthew Dunahoo, Khush Srabony, Rafael Frare, Olivia Slater, Nathan Peel, Maria Kontoyianni, Ken Witt
Somatostatin receptor-4 (SST4) is a therapeutic target for several conditions, including Alzheimer’s disease, seizures, neuropsychiatric disorders, and pain. Our previous work on 1,2,4-triazole derivatives led to enhanced SST4 binding affinity,...
The content of this RSS Feed (c) The Royal Society of Chemistry




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Govt. urged to extend last date to pay crop insurance premium by farmers




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Bids invited for setting up International Dugong Conservation Centre at Manora

The proposed centre, to be set up at an estimate of ₹41 crore, is being established to conserve endangered Dugong species and its habitat in the Palk Bay




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563: Getting Pulled by the Algorithm, AI Training Data, and SVG Drawing

There's a special guest on the show who takes aim at the billionaires in web dev, do we know better than the algorithm for news, why is AI training data such a secret, Chris and Dave discover JetBrains, monorepo struggles, and SVG drawing tools.




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573: Google Reader, Sticky and Overflow, and Figma Thoughts

Chris breaks out his banjo, some thoughts on making music vs recording music, what happened to Google Reader and social reading, what black box properties can't Dave or Chris remember, follow up for dev teams communicating with designers, and what's Adobe going to do about Figma?




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599: Fighting the Algorithm With RSS, Blogging, and the IndieWeb

Dave and Chris discuss indie web culture, the role of social media in today's society, and the challenges and strategies of freelancing. Additionally, they discuss a range of topics from content moderation, coding and refining tech skills, to emerging startups and the future of web technology.




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615: Dave Goes Windows For Real

Dave's got job news to share, as well as insight into the process of what applying for a job in tech is like in 2024. We also talk about styling, scoping, positioning, and floating UI.




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631: Dave’s Second Brain Idea, Notion Thoughts, and Google’s LLM in Chrome

Dave's got an idea for a second brain app that's customized to his brain, where we're at with Notion and other notes apps, and accessibility on LLM's in browsers.




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It’s good ‘office times’ for Bengaluru

The buoyant office market of Bangalore quite makes up for the lukewarm residential segment, according to findings.




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Grey to gold

Use a three-compartment overhead tank to treat greywater.




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Go local is the mantra

Angela Brady, director, Brady Mallalieu Architects, London, tells Nidhi Adlakha why we need to focus on creating sustainable cities with low carbon footprints




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Cargo companies upsize for new business

Booming demand for ecommerce delivery spurs freight handlers to open more centres, digitise for efficiency




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‘Our goal is beauty for each,’ says L’Oréal India chief

Aseem Kaushik, who leads the global beauty giant in India, says tech is playing a big part in its personalisation journey




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Gold loans: Test by fire

Governance, compliance in focus as RBI cautions lenders against lapses




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Govt., BJP spar over Chhath planning as festivities begin today




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Gopal Rai calls meeting over Winter Action Plan progress 




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Several Delhi govt. schemes to tackle toxic air yet to take off

AAP govt. yet to implement at least 5 programmes it announced over the past two years to curb air pollution; these include using drones to map bad air sources and making PUC mandatory to buy fuel; our plans have been stopped by Centre: AAP




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Delhi L-G inspects Gole Market restoration project




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Delhi govt. to start drive against burning of waste in open today

Delhi, neighbouring States likely to experience ‘very poor’ quality air over next 10 days, have placed the depts. concerned on high alert: Gopal Rai




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Chhath Puja: BJP, Cong. slam Delhi govt. over bad air, water




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Delhi govt tests drone-based mist spraying to combat pollution

Pollution levels are elevated at 13 hotspots across Delhi, and this pilot project allows us to test drone-based mist spraying in areas where conventional anti-smog guns can't reach




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Delhi govt okays proposal, 10000 Civil Defence Volunteers to return for anti-pollution work: Atishi

Within two-three days of the registration, the CDVs will be deployed on duties like management of pollution hotspots, preventing dust pollution and garbage burning, she said in a press briefing




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Code is a new form of government: Clive Thompson

The tech journalist and author of Coders explains how programmers have such a huge impact in our everyday lives




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Dialectics of government deficits

The book, espousing modern monetary theory, busts a few conservative myths on government spending




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Dangers of going digital

AI, ML collect loads of user data which can be misused




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Start-up Compass: How Iconic Entrepreneurs got it Right

A relevant book for those about to embark on their entrepreneurial journey, or can serve as a useful resource for those who like to track the start-up ecosystem 




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Goat doctors in Muzaffarpur turn vegetable entrepreneurs

Aga Khan Foundation has given women in this Bihar district a new source of income with state-of-the-art agricultural technology




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MSP law cannot be brought in a hurry; farmers should come forward for talks with govt: Arjun Munda

Union Agriculture Minister Arjun Munda cautioned protesting farmers about some elements usurping their protest for political benefits




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Mango output is set to increase by 14% this year; heat wave unlikely to impact yields

The total production of mangos could jump to 24 million tonnes in the 2023-24 crop year, as against 21 million tonnes in 2022-23




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Mangoes in Tamil Nadu hit by excessive heat, but farmers hopeful

Farmers in Tamil Nadu are struggling with poor yield, but there is also good news with new varieties being discovered




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2024 turns out to be the worst-ever season for mango growers in Rayalaseema in five decades

With over 80% dip in yield following adverse weather conditions, the prospects of earning profits have faded; the situation has turned adverse, as competitors from Telangana and Tamil Nadu started supplying stocks to the pulp units predominantly located in Chittoor district




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Farm loan waivers and elections: How do they affect farmers and governments?

Promises to waive off farm loans have been issued by most political parties during this Lok Sabha election. Here’s a look at how these waivers are implemented, the effect on farmers and governments and what alternatives exist



  • Lok Sabha Elections

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Mango growers demand uniform relief of ₹30,000 per acre, fixed prices at tripartite meeting in Krishnagiri




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In Assam, banks suffer from ‘militancy hangover’: experts

The absence of bank linkage is affecting optimum production by 25 lakh small and marginal farmers in the State, they said




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Budget 2024: Agriculture, Employment, Infrastructure feature in nine priorities of third NDA government

Union Budget 2024 unveils nine priorities for this financial year as Finance Minister Nirmala Sitharaman delivers her seventh budget speech in Lok Sabha




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90-year-old farmer convicted, sentenced to one-year imprisonment for encroaching 36 guntas of government land in Karnataka

Small and marginal farmers are worried about being punished for encroachment, demand action against influential people who allegedly encroached on government land




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M.P. Cabinet increases MSP for soya bean; proposal to go for Centre’s nod




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Kohli the run-machine goes past Tendulkar but...

Kohli's knock of 88 (94) was his 10th 50-plus score in the ODI format this year second only to Shubman Gill who leads the charts with twelve 50-plus ODI scores in 2023.




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'Stats are going out of the window'

'Very pleasing. Most importantly the win, cricket has turned to baseball isn't it? We're delighted with the two points.'




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Godrej Industries net down 16% to Rs. 116 crore




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Demand for petrol cars hits Tiago




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Delay in handover of units from Goa to Daman leaves investors in limbo




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Investment limits for govt. bonds to be auctioned




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Delay over handover of industrial estate from Goa to Daman and Diu leaves investors




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Why is there an upward rally in gold prices? | Explained

Why is gold considered a safety cushion by central banks? When does demand for the yellow metal peak in India? Why does the World Gold Council expect an increased demand for gold from rural areas? What factors determine gold prices?




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Dugong trapped in fishing net rescued, safely released into sea, near Thanjavur district

Forest Department officials said the fishermen who were involved in rescuing the Dugong would be felicitated and rewarded




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Indu Makkal Katchi youth wing president Omkar Balaji questioned for remarks on Nakkheeran Gopal

The Coimbatore police question IMK youth wing leader for threatening to “chop off editor’s tongue”, sparking legal action and protests




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Forest Department free coaching helps tribal youth in Jawadhu Hills to get government jobs