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   Articles with "thapsigargin" as a keyword



Pharmacological preconditioning with the cellular stress inducer thapsigargin protects against experimental sepsis

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recommendations! Published in 2019 at "Pharmacological Research"

DOI: 10.1016/j.phrs.2018.12.017

Abstract: &NA; Previous studies have shown that pretreatment with thapsigargin (TG), a cellular stress inducer, produced potent protective actions against various pathologic injuries. So far there is no information on the effects of TG on the… read more here.

Keywords: sepsis; stress inducer; pharmacological preconditioning; cellular stress ... See more keywords

Rh(I)-Catalyzed Allenic Pauson-Khand Reaction to Access the Thapsigargin Core: Influence of Furan and Allenyl Chloroacetate Groups on Enantioselectivity.

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recommendations! Published in 2022 at "Organic letters"

DOI: 10.1021/acs.orglett.1c03951

Abstract: Thapsigargin (Tg) is a potent SERCA pump inhibitor with the potential to treat cancer and COVID-19. We have extended the scope of the asymmetric allenic Pauson-Khand reaction to furan-tethered allene-ynes, a stereoconvergent transformation affording the… read more here.

Keywords: allenic pauson; pauson khand; khand reaction; thapsigargin ... See more keywords
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Diastereoselective Synthesis of an Advanced Intermediate of Thapsigargin and Other 6,12-Guaianolides Using a RCEYM Strategy.

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recommendations! Published in 2018 at "Organic letters"

DOI: 10.1021/acs.orglett.8b00456

Abstract: A new and flexible approach toward the synthesis of 6,12-guaianolide anticancer drugs such as trilobolides or thapsigargin has been developed that could be applied to the preparation of analogues with a modified ring system. The… read more here.

Keywords: advanced intermediate; intermediate thapsigargin; diastereoselective synthesis; synthesis advanced ... See more keywords

Stereo-Differentiating Asymmetric Rh(I)-Catalyzed Pauson–Khand Reaction: A DFT-Informed Approach to Thapsigargin Stereoisomers

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recommendations! Published in 2024 at "Journal of the American Chemical Society"

DOI: 10.1021/jacs.4c11661

Abstract: We report a stereo-differentiating dynamic kinetic asymmetric Rh(I)-catalyzed Pauson–Khand reaction, which provides access to an array of thapsigargin stereoisomers. Using catalyst-control, a consistent stereochemical outcome is achieved at C2—for both matched and mismatched cases—regardless of… read more here.

Keywords: asymmetric catalyzed; catalyzed pauson; pauson khand; thapsigargin ... See more keywords

Targeting the Activating Mutations of NOTCH1 in T-Cell Lymphoblastic Leukemia with a New SERCA Inhibitor CAD204520

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recommendations! Published in 2019 at "Blood"

DOI: 10.1182/blood-2019-125616

Abstract: Given its oncogenic role in human cancers, Notch1 signaling has garnered increased attention as a therapeutic target. Several Notch modulators, including γ-secretase inhibitors, have shown therapeutic efficacy in preclinical tumor models. However, despite this promise,… read more here.

Keywords: effect; type; leukemia; wild type ... See more keywords