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20 results on '"Lin, Xinglong"'

1. The Current Status and Perspectives of Delivery Strategy for Boronbased Drugs

Author

Yingjun Zhang, Lin Xinglong, Narayan S. Hosmane, Zhu Yinghuai, Jianlin Li, and Hongming Xie

Subjects
inorganic chemicals, medicine.medical_specialty, chemistry.chemical_element, Biochemistry, Bone health, Trade name, 03 medical and health sciences, 0302 clinical medicine, Drug Discovery, medicine, Intensive care medicine, Boron, Clinical treatment, 030304 developmental biology, Pharmacology, 0303 health sciences, Tavaborole, Bortezomib, business.industry, Organic Chemistry, chemistry, 030220 oncology & carcinogenesis, Anti cancer drugs, Molecular Medicine, business, medicine.drug
Abstract

Boron-containing compounds are essential micronutrients for animals and plants despite their low-level natural occurrence. They can strengthen the cell walls of the plants and they play important role in supporting bone health. However, surprisingly, boron-containing compounds are seldom found in pharmaceutical drugs. In fact, there are no inherent disadvantages reported so far in terms of the incorporation of boron into medicines. Indeed, drugs based on boron-containing compounds, such as tavaborole (marked name Kerydin) and bortezomib (trade name Velcade) have been investigated and they are used in clinical treatment. In addition, following the advanced development of boron neutron capture therapy and a new emerging proton boron fusion therapy, more boron-containing medicinals are to be expected. This review discusses the current status and perspectives of delivery strategy for boron-containing drugs.

Published
2019

3. Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors

Author

Bo Chi, Delie An, Lin Xinglong, Yingjun Zhang, Wanrong Dong, Hongming Xie, Fuxing Tan, and Zhihong Peng

Subjects
Pyrimidine, Stereochemistry, Pyridines, Clinical Biochemistry, Pharmaceutical Science, Antineoplastic Agents, Ring (chemistry), 01 natural sciences, Biochemistry, chemistry.chemical_compound, Structure-Activity Relationship, DU145, Cell Line, Tumor, Drug Discovery, Pyridine, Humans, Molecular Biology, IC50, Protein Kinase Inhibitors, Biological evaluation, Cell Proliferation, chemistry.chemical_classification, Dose-Response Relationship, Drug, Molecular Structure, 010405 organic chemistry, Organic Chemistry, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, Enzyme, Pyrimidines, chemistry, Design synthesis, Drug Design, Focal Adhesion Kinase 1, Molecular Medicine, Drug Screening Assays, Antitumor
Abstract

We report herein the synthesis of novel ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors and the evaluation of pharmaceutical activity against five cancer cell lines (MDA-MB-231, BXPC-3, NCI-H1975, DU145 and 786O). Generally, the majority of compounds displayed strong anti-FAK enzymatic potencies (IC50

Published
2020

19. [1,5]-Anion Relay via Intramolecular Proton TransferTo Generate 3,3-Bis(silyl) Allyloxy Lithium: A Useful Scaffold for Syn-Addition to Aldehydes and Ketones.

Author

Lin, Xinglong, Ye, Xincui, Sun, Xianwei, Zhang, Yuebao, Gao, Lu, and Song, Zhenlei

Subjects
*ANIONS, *INTRAMOLECULAR proton transfer reactions, *LITHIUM, *ADDITION reactions, *ALDEHYDES, *KETONES
Abstract

A [1,5]-anionrelay has been achieved in 3,3-bis(silyl) benzylenol ether. Deprotonation at the sterically more accessible benzylposition triggers an intramolecular proton transfer to generate thethermodynamically more stable 3,3-bis(silyl) allyloxy lithium. This endo-oriented allyl anion is stable at −78 °Cand undergoes diastereoselective syn-addition atthe γ-position with aldehydes and ketones to give monobenzyl-substituted1,2-diols. [ABSTRACT FROM AUTHOR]

Published
2014
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20. Bissilyl enal: a useful linchpin for synthesis of functionalized vinylsilane species by anion relay chemistry.

Author

Gao L, Lin X, Lei J, Song Z, and Lin Z

Subjects
Anions chemistry, Molecular Structure, Silanes chemical synthesis, Stereoisomerism, Silanes chemistry, Vinyl Compounds chemical synthesis
Abstract

Bissilyl enal, prepared by a Mannich reaction of 3,3-bissilyl aldehyde with formaldehyde, has proven to be a useful linchpin in an efficient three-component coupling process. The reaction features a [1,4]-Brook rearrangement to generate the silylallyl anion, which adopts a predominant endo-orientation and can undergo addition to electrophiles in a regio- and stereoselective manner, giving various E-vinylsilane species in good yields., (© 2011 American Chemical Society)

Published
2012
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