Zobrazeno 1 - 10 of 43 pro vyhledávání: '"Yingju Xu"'
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Akademický článek
Design, synthesis, and biological evaluation of a novel series of 2-(2,6-dioxopiperidin-3-yl)isoquinoline-1,3(2H,4H)-dione derivatives as cereblon modulators
Autor: Yilin Liu, Yuming Song, Yingju Xu, Meixu Jiang, Haibin Lu
Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 1715-1723 (2022)
In the current study, we designed and synthesised a novel series of 2-(2,6-dioxopiperidin-3-yl)isoquinoline-1,3(2H,4H)-dione derivatives as cereblon (CRBN) modulators. The results of the CCK8 assay revealed potent antiproliferative activity for the s
Externí odkaz: https://doaj.org/article/edb572fb88934f43a73df2318d77159e
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3
Etoposide Amorphous Nanopowder for Improved Oral Bioavailability: Formulation Development, Optimization, in vitro and in vivo Evaluation
Autor: Ping Wang, Shuhang Wang, Yingju Xu, Yue Wang, Sukai Li, Xiangqun Jin, Lu Liu, Mengyan Liu
Publikováno v: International Journal of Nanomedicine. 15:7601-7613
Introduction Etoposide refers to a derivative of podophyllotoxin, which plays an important role in the treatment of cancer due to its prominent anti-tumor effect. As a BCS IV drug, etoposide exhibits insufficient aqueous solubility and permeability,
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::307eec1c56d693a24313d9026dfaafb6
https://doi.org/10.2147/ijn.s265817
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6
Development of an Efficient Route to 2-Ethynylglycerol for the Synthesis of Islatravir
Autor: Tan L, Li D, Wan B, Niki R. Patel, Eric B. Sirota, Xu F, Varsolona Rj, Qi J, Wyvratt Bm, Song Zj, Kuethe Jt, Muzzio Dj, Qiao Z, Chen Y, Yingju Xu, Shang G, Dropinski Jf, Zhang S, Gregory Hughes, Mathew R, Zhao R, Justin A. Newman, Christopher C. Nawrat, Ouyang H, Rummelt Sm, Yin J, Margelefsky E, Kevin M. Maloney
The unnatural, alkyne-containing nucleoside analog islatravir (MK-8591) is synthetically accessed through a biocatalytic cascade starting from 2-ethynylglycerol as a building block. Herein, we describe the development of an efficient synthesis of thi
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::037c4648fcf2256380c2d6d77e9b03d4
https://doi.org/10.26434/chemrxiv.14502744
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7
Synthesis of Islatravir Enabled by a Catalytic, Enantioselective Alkynylation of a Ketone
Autor: Mark A. Huffman, Yingju Xu, Aaron M. Whittaker, Kevin M. Maloney, Teresa Andreani, David M. Tschaen, Andrew Brunskill, François Lévesque, Hongming Li, Christopher C. Nawrat, Mark McLaughlin, Hao Yang, Anna Fryszkowska, Niki R. Patel
Publikováno v: Organic letters. 22(12)
The synthesis of the potent anti-HIV investigational treatment islatravir is described. The key step in this synthesis is a highly enantioselective catalytic asymmetric alkynylation of a ketone. This reaction is a rare example of the asymmetric addit
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8866cb9f28b97cbbb694b890f24515f1
https://pubmed.ncbi.nlm.nih.gov/32516536
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8
Combining traditional 2D and modern physical organic-derived descriptors to predict enhanced enantioselectivity for the key aza-Michael conjugate addition in the synthesis of Prevymis™ (letermovir)
Autor: Guy R. Humphrey, Katrina W. Lexa, Cheol K. Chung, Celine B. Santiago, Zhijian Liu, Edward C. Sherer, Rebecca T. Ruck, Toni T. Metsänen, Yingju Xu, Matthew S. Sigman
Publikováno v: Chemical Science. 9:6922-6927
Quantitative structure–activity relationships have an extensive history for optimizing drug candidates, yet they have only recently been applied in reaction development. In this report, the predictive power of multivariate parameterization has been
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f99a9db15e5ff2edfb385a44c364d97b
https://doi.org/10.1039/c8sc02089b
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9
Asymmetric Hydrogen Bonding Catalysis for the Synthesis of Dihydroquinazoline-Containing Antiviral, Letermovir
Autor: Katrina W. Lexa, Daniel A. DiRocco, Zhijian Liu, Cheol K. Chung, Rebecca T. Ruck, Yining Ji, Teresa Andreani, Guy R. Humphrey, Yingju Xu
Publikováno v: Journal of the American Chemical Society. 139:10637-10640
A weak Bronsted acid-catalyzed asymmetric guanidine aza-conjugate addition reaction has been developed. C2-symmetric, dual hydrogen-bond donating bistriflamides are shown to be highly effective in activating α,β-unsaturated esters toward the intram
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::598afcd8a949fdf466122fd904a75248
https://doi.org/10.1021/jacs.7b05806
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10
Protein targeting chimeric molecules specific for dual bromodomain 4 (BRD4) and Polo-like kinase 1 (PLK1) proteins in acute myeloid leukemia cells
Autor: Haibin Lu, Yingju Xu, Jingyao Wang, Xupeng Mu, Liting Bai
Publikováno v: Biochemical and biophysical research communications. 521(4)
Proteolysis targeting chimeras (PROTACs) are hetero-bifunctional molecules that could simultaneously bind to the target protein and the E3 ubiquitin ligase, thereby leading to selective degradation of the target protein. Polo-like kinase 1 (PLK1) and
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ff9465bf4373880ad52fe22b63109190
https://pubmed.ncbi.nlm.nih.gov/31708096
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