[Supplement] Design, synthesis, and biological evaluation of thieno[2,3-d]pyrimidine derivatives as novel dual c-Met and VEGFR-2 kinase inhibitors

DOI : 10.1016/j.bmc.2017.11.010

URL : https://www.sciencedirect.com/science/article/pii/S096808961731790X

Thanks!!

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๐Ÿ‘ค︎ u/snirtyscientist
๐Ÿ“…︎ Nov 27 2018
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Non-Small Cell Lung Cancer (NSCLC) Drugs Market Forecast 2017-2027: Chemotherapy, EGFR and ALK Inhibitors, VEGF/VEGFR Inhibitors, Immunotherapy, Other globenewswire.com/news-reโ€ฆ
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๐Ÿ‘ค︎ u/montaukwhaler
๐Ÿ“…︎ Sep 13 2017
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Intranasal inhibitor blocks omicron and other variants of SARS-CoV-2 researchsquare.com/articlโ€ฆ
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๐Ÿ‘ค︎ u/RufusSG
๐Ÿ“…︎ Dec 28 2021
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Revive Therapeutics Announces Published Research Results on Bucillamine as Potential Inhibitor of SARS-CoV-2 Infection Delta Variant globenewswire.com/news-reโ€ฆ
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๐Ÿ‘ค︎ u/supergarvis
๐Ÿ“…︎ Nov 16 2021
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MyMD to commence Phase 2 trial in frailty Pharma start-up targets #sarcopenia with TNF inhibitor; claims compelling lifespan extension and frailty results in mice.

https://www.longevity.technology/mymd-to-commence-phase-2-trial-in-frailty/?utm_source=reddit&utm_medium=social&utm_campaign=frail

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๐Ÿ‘ค︎ u/philnewman100
๐Ÿ“…︎ Dec 14 2021
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Australian biotech starting phase 2 FAK inhibitor trail recruitment in Q1 2022. reddit.com/gallery/rtbw5y
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๐Ÿ‘ค︎ u/Rob2moon
๐Ÿ“…︎ Jan 01 2022
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New University of Glasgow Preprint study shows SARS-COV-2 Omicron variant has switched preference for cell entry from TMPRSS2 mediated pathway to endosomal pathway thereby increasing effectiveness of endosomal entry inhibitors like HCQ (link: https://www.gla.ac.uk/media/Media_829360_smxx.pdf)
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๐Ÿ“…︎ Jan 04 2022
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Glutathione as a potent inhibitor against SARS CoV-2 Main protease: Molecular docking and dynamics simulations osf.io/tpeja/
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๐Ÿ‘ค︎ u/Biomedical_trader
๐Ÿ“…︎ Nov 19 2021
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Do you want season 2 to continue exploring what inhibitor chips are and what they're capable of?

We learned a lot about the inhibitor chips in season 1 like how they can be activated, how they shut down the personality of clones, and how they don't always work like they're supposed to. Is there more you want to know about them in season 2 or do you want the BB to move on from them?

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๐Ÿ“…︎ Nov 12 2021
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hello guys i am reading the article and i have question here . 1. what is the negative value of interactions engergy ? 2.why Planar geometry leads to more strength the interactions between inhibitors and the Al ? 3. why does longer โ„ซ can tell us its more stable shape? sorry about this many questions reddit.com/gallery/rcfvm2
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๐Ÿ‘ค︎ u/Germuny
๐Ÿ“…︎ Dec 09 2021
๐Ÿšจ︎ report
$COCP Cocrystal Pharmaโ€™s COVID-19 Oral and Intranasal/Pulmonary Protease Inhibitors Exhibit Powerful Potency Against the SARS-CoV-2 Omicron Variant

>To confirm the antiviral activity of its protease inhibitors against SARS-CoV-2 Omicron variant, Cocrystal conducted an analysis of SARS-CoV-2 lineages covering all reported Omicron variant sequences including those from South Africa, Europe, Asia and North America, and identified one prevalent mutation in the SARS-CoV-2 main protease. Using its proprietary platform technology and assays, the Company further confirmed in vitro antiviral activity of its protease inhibitors against the Omicron variant.
>
>the Company plans to begin a Phase 1 study also as rapidly as possible with an orally administered protease inhibitor.

https://www.sec.gov/Archives/edgar/data/1412486/000149315221032236/ex99-1.htm

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๐Ÿ‘ค︎ u/-mylankovic-
๐Ÿ“…︎ Dec 22 2021
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Comment and response on "Capillary Ketone Concentrations at the Time of Colonoscopy: A Cross-Sectional Study With Implications for SGLT2 Inhibitor-Treated Type 2 Diabetes"

Arguing on the cut-off level to detect ketoacidosis in type 2 diabetics on SGLT2i undergoing colonoscopy.

original publication:

https://www.reddit.com/r/ketoscience/comments/mznaav/capillary_ketone_concentrations_at_the_time_of/

comment:

https://diabetesjournals.org/care/article/45/1/e15/139159/Comment-on-Hamblin-et-al-Capillary-Ketone

...

The study on sodiumโ€“glucose cotransporter 2 inhibitor (SGLT2i) therapy by Hamblin et al. (1) advocates for increasing ฮฒ-hydroxybutyrate (BHB) to 1.7 mmol/L for hyperketonemia, in contrast to our previously suggested threshold of 1.0 mmol/L (2). This change is premature, since the new cutoff is based on a nonnormally distributed data set, the risk of developing ketoacidosis is different in patients with diabetes compared with patients without diabetes, and a higher BHB threshold may increase the false-negative rate of early ketoacidosis.

...

response:

https://diabetesjournals.org/care/article/45/1/e17/139144/Response-to-Comment-on-Hamblin-et-al-Capillary

...

The cutoff for ฮฒ-hydroxybutyrate concentrations of >1.0 mmol/L is not evidence-based. This was the very reason we undertook our study. Many colonoscopies are carried out in day procedure centers where there is no access to on-site blood gas analyzers or expertise for dextrose-insulin infusions. If the ketone concentration cutoff of >1.0 mmol/L is used, a significant proportion of people would have their procedure canceled, given that 9% of normoglycemic individuals and 24% of sodiumโ€“glucose cotransporter 2 inhibitor (SGLT2i)-treated participants in our study had ketone levels >1.0 mmol/L. The very small risk of diabetic ketoacidosis (DKA) in SGLT2i-treated people undergoing colonoscopy must be balanced by potential delays in detecting and treating colorectal cancer. This is a real concern, given that a recent population-based study showed prediagnostic colonoscopies are associated with 17% lower risk of death from colorectal cancer (4).

...

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๐Ÿ‘ค︎ u/Ricosss
๐Ÿ“…︎ Jan 06 2022
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Revive Therapeutics Announces Published Research Results on Bucillamine as Potential Inhibitor of SARS-CoV-2 Infection Delta Variant globenewswire.com/news-reโ€ฆ
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๐Ÿ‘ค︎ u/SignalChoice
๐Ÿ“…︎ Nov 16 2021
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Exploring the Binding Mechanism of PF-07321332 SARS-CoV-2 Protease Inhibitor through Molecular Dynamics and Binding Free Energy Simulations - PubMed pubmed.ncbi.nlm.nih.gov/3โ€ฆ
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๐Ÿ‘ค︎ u/thonioand
๐Ÿ“…︎ Dec 23 2021
๐Ÿšจ︎ report
Looking for experiences with 2 MAOI Inhibitors and the acacia

I have a chance to work with this medicine this weekend. The facilitator says he has had a big download of information and feels like he can consider himself a practitioner. I thought it was going to be ayahuasca. He says this is a similar experience. Just getting a feel for what Iโ€™m in for. Iโ€™ve been pretty good about following the same diet I had for my last Ayahuasca experiences. โœŒ๏ธ โค๏ธ

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๐Ÿ‘ค︎ u/Dchongo
๐Ÿ“…︎ Dec 14 2021
๐Ÿšจ︎ report
The relentless search for SARS-CoV-2 Mแต–สณแต’ inhibitors: Validation and invalidation of SARS-CoV-2 main protease inhibitors using the Flip-GFP and Protease-Glo luciferase assays
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๐Ÿ‘ค︎ u/Badatu
๐Ÿ“…︎ Nov 14 2021
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An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19 science.org/doi/10.1126/sโ€ฆ
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๐Ÿ‘ค︎ u/RufusSG
๐Ÿ“…︎ Nov 03 2021
๐Ÿšจ︎ report
Todos Medical Announces Completion of Enrollment for COVID-19 Oral Antiviral 3CLPro (Mpro) Inhibitor Tollovir Phase 2 Clinical Trial Interim Analysis in Severe and Critical Hospitalized Patients

https://investor.todosmedical.com/news-events/press-releases/detail/153/todos-medical-announces-completion-of-enrollment-for

Enrollment now paused in the randomized, double blind, placebo controlled clinical trial in severe and critical hospitalized COVID-19 patients to complete interim analysis

Data from the interim analysis expected in the end of 4th Quarter of 2021 Jules Mitchel, PhD, appointed as strategic advisor to assist with the interim analysis

New York, NY, and Tel Aviv, ISRAEL, Nov. 19, 2021 (GLOBE NEWSWIRE) -- viaย NewMediaWire --

Todos Medical, Ltd.(TOMDF), a comprehensive medical diagnostics and related solutions company, together with its 3CL protease biology-focused joint venture partner NLC Pharma, Ltd., today is very pleased announce an update regarding the ongoing clinical development of Tollovirยฎ, a oral antiviral 3CL protease (3CLpro, Main protease, Mpro, Nsp5) inhibitor & anti-cytokine therapeutic candidate for the treatment of COVID-19. The enrollment of the 77-patient, Phase 2, randomized, double-blind, placebo controlled clinical trial in hospitalized COVID-19 patients has been paused at the two open clinical sites in Israel, Shaare Zedek Medical Center in Jerusalem and Hillel Yaffe Medical Center in Hadera, to allow for an interim analysis of the data. The Company expects data from the interim analysis to be reviewed by the trial Data Safety and Monitoring Board (DSMB) in the fourth quarter of 2021.

Concurrent with this announcement, the Company announced that it has retained the services of Jules Mitchel, PhD, to assist the Company with the interim analysis. Dr. Mitchel has an extensive background in the clinical trial and regulatory affairs space, previously serving as Founder & CEO of global clinical research organization (CRO) Target Health from its founding in 1993 until it was sold to dMed Biopharmaceuticals in 2019.

The interim analysis, previously scheduled to occur at 33 patients, will now be conducted on the 31 patients enrolled in the trial as of November 10, 2021 based on the recommendation from the statistician using blinded data that indicated the clinical trial has likely met the threshold required to evaluate futility.

The primary endpoints for the trial are:

Reduction in the duration of hospitalization

Time to clinical improvement as

... keep reading on reddit โžก

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๐Ÿ‘ค︎ u/Diligent_Cause
๐Ÿ“…︎ Nov 19 2021
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High-Throughput Activity Assay for Screening Inhibitors of the SARS-CoV-2 Mac1 Macrodomain pubs.acs.org/doi/10.1021/โ€ฆ
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๐Ÿ‘ค︎ u/Peeecee7896
๐Ÿ“…︎ Dec 15 2021
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Tonix Pharmaceuticals Announces Publication of Paper on Antiviral SARS-CoV-2 Inhibitor, TNX-3500, in JCI Insight globenewswire.com/en/newsโ€ฆ
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๐Ÿ‘ค︎ u/ivanshim
๐Ÿ“…︎ Dec 01 2021
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Exploring the Binding Mechanism of PF-07321332 SARS-CoV-2 Protease Inhibitor through Molecular Dynamics and Binding Free Energy Simulations mdpi.com/1422-0067/22/17/โ€ฆ
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๐Ÿ‘ค︎ u/SecretAgentIceBat
๐Ÿ“…︎ Nov 30 2021
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Sitagliptin - First In Class DPP4 Inhibitor for Type 2 Diabetes us.huatengsci.com/news/shโ€ฆ
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๐Ÿ‘ค︎ u/sunnyfang14
๐Ÿ“…︎ Dec 17 2021
๐Ÿšจ︎ report
A highly sensitive cell-based luciferase assay for high-throughput automated screening of SARS-CoV-2 nsp5/3CLpro inhibitors biorxiv.org/content/10.11โ€ฆ
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๐Ÿ‘ค︎ u/sburgess86
๐Ÿ“…︎ Dec 21 2021
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Blood pressure drugs could prevent Type 2 diabetes. In the largest study of its kind, researchers found angiotensin-converting enzyme (ACE) inhibitors and angiotensin II receptor blockers (ARBs) had the strongest protective effect, reducing someoneโ€™s relative risk of developing diabetes by 16%. thelancet.com/journals/laโ€ฆ
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๐Ÿ‘ค︎ u/morenewsat11
๐Ÿ“…︎ Nov 12 2021
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Looking for experiences with 2 MAOI Inhibitors and the acacia /r/Psychonaut/comments/rgโ€ฆ
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๐Ÿ‘ค︎ u/Dchongo
๐Ÿ“…︎ Dec 14 2021
๐Ÿšจ︎ report
The relentless search for SARS-CoV-2 Mแต–สณแต’ inhibitors: Validation and invalidation of SARS-CoV-2 main protease inhibitors using the Flip-GFP and Protease-Glo luciferase assays (Nov 2021) sciencedirect.com/scienceโ€ฆ
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๐Ÿ‘ค︎ u/Badatu
๐Ÿ“…︎ Nov 14 2021
๐Ÿšจ︎ report
Characterization of the non-covalent interaction between the PF-07321332 inhibitor and the SARS-CoV-2 main protease sciencedirect.com/scienceโ€ฆ
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๐Ÿ‘ค︎ u/SecretAgentIceBat
๐Ÿ“…︎ Nov 30 2021
๐Ÿšจ︎ report
The relentless search for SARS-CoV-2 Mแต–สณแต’ inhibitors ( อกยฐ อœส– อกยฐ) Article: Validation and invalidation of SARS-CoV-2 main protease inhibitors using the Flip-GFP and Protease-Glo luciferase assays
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๐Ÿ‘ค︎ u/Badatu
๐Ÿ“…︎ Nov 11 2021
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