Huan‐Qiu Li

Soochow University

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Hai‐Liang Zhu

Nanjing University

Zhu‐Ping Xiao

Jishou University

Lei Shi

China Pharmaceutical University

Rui-Qin Fang

University of Electronic Science and Technology of China

Hai‐Liang Zhu

Northwestern Polytechnical University

Jia‐Yu Xue

Nanjing Agricultural University

Peng‐Cheng Lv

Southwest Jiaotong University

Ying Yang

Stanford University

Eddine Saiah

Pfizer (United States)

Yin Luo

Henan University of Technology

Cooperative Institutions

AbbVie (United States)

Nanjing University

Pfizer (United States)

Soochow University

Inflammation Research Foundation

University of Toronto

Abbott Fund

China Pharmaceutical University

Structural Genomics Consortium

Chinese Academy of Sciences

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1,4,8,11-Tetrakis(carboxymethyl)-5,5,7,12,12,14-hexamethyl-1,4,8,11-tetraazoniacyclotetradecane tetrachloride octahydrate

Acta Crystallographica Section E Structure Reports Online (2005)

Shifan Wang Huan‐Qiu Li Ban-Feng Ruan Hai‐Liang Zhu Seik Weng Ng

The crystal structure of the centrosymmetric title compound, C24H48N4O84+·4Cl−·8H2O, consists of a 14-membered methyl-substituted C10N4 cationic ring which interacts with the chloride ions and water molecules of crystallization to give a three-dimensional hydrogen-bonded network structure.

Cationic polymerization

Tetrachloride

10.1107/s1600536805020817

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Design, synthesis and structure–activity relationships of antiproliferative 1,3-disubstituted urea derivatives

European Journal of Medicinal Chemistry (2008)

Huan‐Qiu Li Tao‐Tao Zhu Tao Yan Yin Luo Hai‐Liang Zhu

MTT assay

Structure–activity relationship

10.1016/j.ejmech.2008.04.011

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Citations (34)

Urea Derivatives as Anticancer Agents

Anti-Cancer Agents in Medicinal Chemistry (2009)

Huan‐Qiu Li Peng‐Cheng Lv Tao Yan Hai‐Liang Zhu

Within the past ten years, a huge volume of research on the synthesis, structure-activity relationships (SAR), and anticancer activities of the urea derivatives was reported. Many aromatic urea derivatives such as N-phenyl-N-(2-chloroethyl)ureas (CEUs) and benzoylureas (BUs) show good anticancer activity, and these compounds have mainly been proved to be tubulin ligands that inhibit the polymerization of tubulin. Heterocyclic urea derivatives play an important role in anticancer agents because of their good inhibitory activity against receptor tyrosine kinases (RTKs), raf kinases, protein tyrosine kinases (PTKs), and NADH oxidase, which play critical roles in many aspects of tumorigenesis. Thiourea derivatives are also of wide interest because of their diverse anticancer activity against various leukemias and solid tumors. In this review, the anticancer activity of the urea derivatives mentioned above is summarized in detail. It is hoped that increasing knowledge of the SAR and cellular processes underlying the antitumor-activity of urea derivatives will be beneficial to the rational design of new generation of urea anticancer drugs.

Rational design

10.2174/1871520610909040471

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Inhibitors of Tumor Progression Loci-2 (Tpl2) Kinase and Tumor Necrosis Factor α (TNF-α) Production: Selectivity and in Vivo Antiinflammatory Activity of Novel 8-Substituted-4-anilino-6-aminoquinoline-3-carbonitriles

Journal of Medicinal Chemistry (2007)

Neal Green Yonghan Hu Kristin Janz Huan‐Qiu Li Neelu Kaila

Tumor progression loci-2 (Tpl2) (Cot/MAP3K8) is a serine/threonine kinase in the MAP3K family directly upstream of MEK. Recent studies using Tpl2 knockout mice have indicated an important role for Tpl2 in the lipopolysaccharide (LPS) induced production of tumor necrosis factor alpha (TNF-alpha) and other proinflammatory cytokines involved in diseases such as rheumatoid arthritis. Initial 4-anilino-6-aminoquinoline-3-carbonitrile leads showed poor selectivity for Tpl2 over epidermal growth factor receptor (EGFR) kinase. Using molecular modeling and crystallographic data of the EGFR kinase domain with and without an EGFR kinase-specific 4-anilinoquinazoline inhibitor (erlotinib, Tarceva), we hypothesized that we could diminish the inhibition of EGFR kinase by substitution at the C-8 position of our 4-anilino-6-aminoquinoline-3-carbonitrile leads. The 8-substituted-4-anilino-6-aminoquinoline-3-carbonitriles were prepared from the appropriate 2-substituted 4-nitroanilines. Modifications to the C-6 and C-8 positions led to the identification of compounds with increased inhibition of TNF-alpha release from LPS-stimulated rat and human blood, and these analogues were also highly selective for Tpl2 kinase over EGFR kinase. Further structure-activity based modifications led to the identification of 8-bromo-4-(3-chloro-4-fluorophenylamino)-6-[(1-methyl-1H-imidazol-4-yl)methylamino]quinoline-3-carbonitrile, which demonstrated in vitro as well as in vivo efficacy in inhibition of LPS-induced TNF-alpha production.

Proinflammatory cytokine

10.1021/jm070436q

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Citations (45)

Synthesis, biological evaluation and molecular docking studies of amide-coupled benzoic nitrogen mustard derivatives as potential antitumor agents

Bioorganic & Medicinal Chemistry (2009)

Qing‐Zhong Zheng Fei Zhang Kui Cheng Ying Yang Yu Chen

Docking (animal)

Nitrogen mustard

Amide

Benzoic acid

Molecular model

10.1016/j.bmc.2009.11.037

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Citations (21)

DNA Methyltransferase Inhibitors and their Therapeutic Potential

Current Topics in Medicinal Chemistry (2018)

Zehao Zhou Huan‐Qiu Li Feng Liu

Aberrant DNA methylation at the 5-position of cytosine, catalyzed by DNA methyltransferases (DNMTs), is associated with not only various cancers by silencing of tumor suppressor genes but also other diseases. The DNMTs, especially the DNMT1, DNMT3A and DNMT3B, are often overexpressed in various cancer tissues and cell lines. DNMTs are important epigenetic targets for drug development since the DNA methylation is reversible. This review summarizes an array of nucleoside and non-nucleoside inhibitors of DNMTs, as well as their biological activities. Among these inhibitors, the nucleoside analogue azacytidine and its deoxy derivative decitabine are both irreversible DNMT inhibitors and approved for the treatment of myelodysplastic syndrome.

Decitabine

DNMT3B

DNMT1

Azacitidine

DNA methyltransferase

Cytosine

10.2174/1568026619666181120150122

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Citations (78)

CCDC 663761: Experimental Crystal Structure Determination

The Cambridge Structural Database (2007)

Zhu‐Ping Xiao Rui-Qin Fang Huan‐Qiu Li Hai‐Liang Zhu

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, cell parameters, space group, experimental conditions and quality measures.

10.5517/ccq8pn9

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5,7-Dimethoxy-3-(4-methoxyphenyl)-4H-chromen-4-one

Acta Crystallographica Section E Structure Reports Online (2007)

Huan‐Qiu Li Zhu‐Ping Xiao Yue Han Rui-Qin Fang Hai‐Liang Zhu

In the genistein-related title molecule, C18H16O5, the dihedral angle between the two benzene rings is 59.25 (6)°.

10.1107/s1600536807041773

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Citations (1)

The Syntheses and Crystal Structures of Metronidazole-derived Compounds

Journal of Chemical Crystallography (2008)

Huan‐Qiu Li Zhu‐Ping Xiao Rui-Qin Fang Hai‐Liang Zhu

Triclinic crystal system

Monoclinic crystal system

Organometallic Chemistry

10.1007/s10870-008-9343-9

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Citations (6)

Synthesis and Cytotoxic Evaluation of a Series of Genistein Derivatives

Chemistry & Biodiversity (2006)

Huan‐Qiu Li Hui Ming Ge Yun‐Xi Chen Chen Xu Lei Shi

Abstract Thirty genistein (=5,7‐dihydroxy‐3‐(4‐hydroxyphenyl)‐4 H ‐1‐benzopyran‐4‐one; GEN) derivatives were synthesized from genistein through a facile approach in high yields. Compounds 9, 11, 12, 23 – 30 were reported for the first time, while 13 – 22 have already been reported in our recent paper. The cytotoxic activities of these compounds were evaluated against a human nasopharyngeal epidermoid tumor cell line KB. Compounds 7 – 9, 12, 14, 16 – 19, 21, 24, 27, 29 showed remarkable antitumor activities in vitro , which was comparable with 5‐fluorouracil, an anticancer drug. On the basis of the obtained experimental data, structure–effect relationships were discussed.

Benzopyrans

10.1002/cbdv.200690049

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Citations (23)