Dali Yin

Chinese Academy of Medical Sciences & Peking Union Medical College

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Xiaojian Wang

Chinese Academy of Medical Sciences & Peking Union Medical College

Qiong Xiao

Chinese Academy of Medical Sciences & Peking Union Medical College

Yulin Tian

Chinese Academy of Medical Sciences & Peking Union Medical College

Xiaoguang Chen

China University of Petroleum, East China

Haihong Huang

Chinese Academy of Medical Sciences & Peking Union Medical College

Jinping Hu

Chinese Academy of Medical Sciences & Peking Union Medical College

Jianguo Qi

Chinese Academy of Medical Sciences & Peking Union Medical College

Huaqing Cui

Chinese Academy of Medical Sciences & Peking Union Medical College

Jing Jin

Peking Union Medical College Hospital

Zeyu Shi

University of Hong Kong

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Chinese Academy of Medical Sciences & Peking Union Medical College

146

Peking Union Medical College Hospital

Peking University

Chinese Academy of Sciences

Capital Medical University

Shanghai Jiao Tong University

Sichuan University

Zhejiang University

Academy of Medical Sciences

Sun Yat-sen University

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Synthesis of tetrahydroisoquinolines through TiCl4-mediated cyclization and Et3SiH reduction

Chinese Chemical Letters (2019)

Zeyu Shi Qiong Xiao Dali Yin

Sequence (biology)

Derivative (finance)

10.1016/j.cclet.2019.09.023

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Citations (6)

Development of a selective S1P1 receptor agonist, Syl930, as a potential therapeutic agent for autoimmune encephalitis

Biochemical Pharmacology (2014)

Jing Jin Jinping Hu Wanqi Zhou Xiaojian Wang Qiong Xiao

Sphingosine-1-phosphate receptor

Autoimmune encephalitis

Neuroimmunology

10.1016/j.bcp.2014.04.010

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Citations (25)

Cover Picture: Structural Simplification of Bedaquiline: the Discovery of 3-(4-(N ,N -Dimethylaminomethyl)phenyl)quinoline-Derived Antitubercular Lead Compounds (ChemMedChem 2/2017)

ChemMedChem (2017)

Chun‐Xian He Laura Preiß Bin Wang Lei Fu Hui Wen

The front cover picture shows a molecular model of a bacterial rotary ATP synthase, which is targeted and inhibited by the novel antituberculosis (TB) drug Bedaquiline (Sirturo®), the first anti-TB antibiotic compound in 40 years. Bedaquiline synthesis is expensive, mainly due to two chiral centers within the molecule. Using a fragment based synthesis approach He, Preiss et al. present an economical way of producing Bedaquiline derivatives with no chiral centers that still maintain antitubercular activity against Mycobacterium tuberculosis. More information can be found in the Full Paper by Huaqing Cui, Thomas Meier, Dali Yin et al. on page 106 in Issue 2, 2017 (DOI: 10.1002/cmdc.201600441). (The picture was drawn by Dr. Laura Preiss.)

Bedaquiline

Quinoline

Front cover

10.1002/cmdc.201600625

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Synthesis and anti-tubercular activity of novel alkyl substituted riminophenazine derivatives.

PubMed (2012)

Yuli Li Chunlin Zhang Dongfeng Zhang Yu Lu Bin Wang

A series of novel riminophenazine derivatives bearing an alkyl substituent attached to N-5 and imino nitrogen at C-3 position of the phenazine ring were obtained through rational drug design, aiming to maintain high anti-tubercular activity, lower toxicity and reduce lipophilicity. All target compounds were prepared by utilizing simple and flexible synthetic route and evaluated against Mycobacterium tuberculosis H37Rv and screened for mammalian cytotoxicity. The results demonstrated that compounds with a cyclopropyl substituent at N-5 position were more active than the reference compound clofazimine. In particular, 2-(4-chloroanilino)-5-cyclopropyl-3-(4-methoxycyclohexyl) imino-3, 5-dihydrophenazine (25) was found to be the most potent compound with low cytotoxicity and lipophilicity. This compound could serve as a valuable lead molecule for further optimization.

Lipophilicity

Lead compound

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Citations (5)

Synthesis and bio-evaluation of phenothiazine derivatives as new anti-tuberculosis agents

Chinese Chemical Letters (2015)

Chun‐Xian He Hui Meng Xiang Zhang Huaqing Cui Dali Yin

10.1016/j.cclet.2015.03.027

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Citations (22)

Four new minor taxanes from cell cultures ofTaxus chinensis

Journal of Asian Natural Products Research (2009)

Dan Xie Hongting Jia Yi Zhang Jianhua Zou Dali Yin

Four new minor taxanes (1-4) have been isolated from Ts-19 cell cultures of Taxus chinensis together with five known taxanes (5-9) by silica gel chromatography combined with semi-preparative HPLC chromatography. On the basis of the analyses of the chemical and spectroscopic (IR, MS, 1D, and 2D NMR) data, the structures of new compounds were elucidated as 5alpha-hydroxy-2alpha,10beta-diacetoxy-14beta-(3-hydroxy-2-methyl-butyryl)oxytaxa-4(20),11-diene (1), 2alpha,5alpha,10beta-triacetoxy-14beta-(2-hydroxy-propionyl)oxytaxa-4(20),11-diene (2), 2alpha,5alpha,10beta-triacetoxy-14beta-(2-hydroxy-3-methyl-butyryl)oxytaxa-4(20),11-diene (3), and 2alpha-benzoxy-4alpha,9alpha,10beta,13alpha-tetraacetoxytax-11-ene (4), respectively. Compounds 1-5 were pharmacologically evaluated for their cytotoxicities against five human cancer cell lines (HCT-8, Bel-7402, BGC-823, A549, and A2780) and their reversing activity towards multi-drug resistance A549/taxol tumor cell line, and the results showed that all of the tested compounds exhibited very low cytotoxicities, while compound 4 possessed twice the reversing activity as that of verapamil at 10 muM.

Cancer cell lines

Chemical structure

10.1080/10286020902882143

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Citations (4)

Diversity-Oriented Synthesis of Heterocycles: Al(OTf)₃-Promoted Cascade Cyclization and Ionic Hydrogenation

The Journal of Organic Chemistry (2018)

Tianqi Liu Wen‐Qiang Jia Qiumu Xi Yonghui Chen Xiaojian Wang

An efficient and facile method has been developed for the diversity-oriented synthesis of heterocycles. Hexahydrophenoxazines, tetrahydroquinolines, indolines, hexahydrocarbazoles, and lactones were conducted via Al(OTf)3-promoted cascade cyclization and ionic hydrogenation. Furthermore, this protocol was utilized to smoothly prepare piracetam and its key intermediate as well.

Cascade reaction

10.1021/acs.joc.7b02894

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Citations (17)

Ti(iv)-catalyzed cascade synthesis of tetrahydrofuro[3,2-d]oxazole from arene-1,4-diones

Organic & Biomolecular Chemistry (2015)

Gang Li Li Li Haihong Huang Dali Yin

The tandem ionic hydrogenation, ketalization, and intramolecular cyclization of arene-1,4-diones with a combination of TiCl₄/Et₃SiH give facile access to tetrahydrofuro[3,2-d]oxazole derivatives in good yields at room temperature.

Oxazole

10.1039/c5ob00174a

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Citations (3)

ChemInform Abstract: One‐Pot Synthesis of Dibenzodiazepinones via CuI Catalysis in Ethylene Glycol.

ChemInform (2013)

Qingyang Zhang Xiaojian Wang Yulin Tian Jianguo Qi Chun Li

10.1002/chin.201352198

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Citations (0)

ChemInform Abstract: Ti(IV)‐Catalyzed Cascade Synthesis of Tetrahydrofuro[3,2‐d]oxazole from Arene‐1,4‐diones.

ChemInform (2015)