Xijun Sheng

Organocatalytic Higher-Order [8+2] Cycloaddition for the Assembly of Atropoenantiomeric 3-Arylindolizines

Gongming Yang, Zhipeng Li, Yuhan Liu, Donghui Guo et autres

We present an unprecedented atroposelective [8+2] cycloaddition reaction between pyridinium/isoquinolinium ylides and ynals. It is worth noting that this protocol represents a new example of the organocatalyzed atropoenantioselective higher-order cycloaddition reaction, providing various axial chiral 3-arylindolizines in good yields and high enantioselectivities. …

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CCDC 2102971: Experimental Crystal Structure Determination

Gongming Yang, Zhipeng Li, Yuhan Liu, Donghui Guo et autres

Discovery and Evaluation of Pyrazolo[3,4-d]pyridazinone as a Potent and Orally Active Irreversible BTK Inhibitor

Xuejun Zhang, Xijun Sheng, Jie Shen, Shoubo Zhang et autres

The identification and lead optimization of a series of pyrazolo[3,4- d ]pyridazinone derivatives are described as a novel class of potent irreversible BTK inhibitors, resulting in the discovery of compound 8 . Compound 8 exhibited high potency against BTK kinase and acceptable …

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後成的ポリコム抑制複合体2(PRC2)メチルトランスフェラーゼをアロステリック阻害するEEDバインダーの構造ガイドデザイン

Andreas Lingel, Martin Sendzik, Huang Ying, D Shultz Michael et autres

Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Methyltransferase PRC2

Andreas Lingel, Dirksen E. Bussiere, John Cantwell, Michael P. Dillon et autres

PRC2 is a multisubunit methyltransferase involved in epigenetic regulation of early embryonic development and cell growth. The catalytic subunit EZH2 methylates primarily lysine 27 of histone H3, leading to chromatin compaction and repression of tumor suppressor genes. Inhibiting this activity by small …

Structure-Guided Design of EED Binders Allosterically Inhibiting the Epigenetic Polycomb Repressive Complex 2 (PRC2) Methyltransferase

Andreas Lingel, Martin Sendzik, Ying R. Huang, Michael D. Shultz et autres

PRC2 is a multisubunit methyltransferase involved in epigenetic regulation of early embryonic development and cell growth. The catalytic subunit EZH2 methylates primarily lysine 27 of histone H3, leading to chromatin compaction and repression of tumor suppressor genes. Inhibiting this activity by small …

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Synthesis and Biological Activity of 4‐[(Substituted Phenoxyacetoxy)methyl]‐2,6,7‐trioxa‐1‐phosphabicyclo[2.2.2]octane‐1‐one

Xijun Sheng, Yuan Zhou, Shasha Zhang, Hao Peng et autres

A series of novel 4‐[(substituted phenoxyacetoxy)methyl]‐2,6,7‐trioxa‐1‐phosphabicyclo[2.2.2]octane‐1‐one 4a, 4b, 4c, 4d, 4e, 4f, 4g, 4h, 4i, 4j, 4k, 4l, 4m, 4n, 4o were synthesized. Their structures were confirmed by IR, 1H NMR, mass spectroscopy, and elemental analyses. The results of preliminary bioassays show …

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4-[(2-Chloro-5-methylphenoxy)acetoxymethyl]-2,6,7-trioxa-1-phosphabicyclo[2.2.2]octane 1-oxide

Xijun Sheng, Hongwu He

In the structure of the title compound, C14H16ClO7P, the P atom is in a distorted tetra­hedral configuration. The data reveal that some strain is probably present in the bicyclic structure. The terminal O=P bond distance is 1.4426 (16) Å, and the bridging …

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5,5-Dimethyl-2-(naphthalen-1-yloxy)-1,3,2-dioxaphosphinane 2-oxide

Zhengqiu Li, Xijun Sheng, Na Zuo, Qingyun Ren et autres

In the crystal structure of the title compound, C15H17O4P, mol­ecules are linked into chains by C—H⋯O hydrogen bonds.

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CCDC 624511: Experimental Crystal Structure Determination

Xijun Sheng, Hongwu He

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …