Chemical Biology & Drug Design

Cover image for Vol. 85 Issue 3

Accepted Articles (Accepted, unedited articles published online and citable. The final edited and typeset version of record will appear in future.)

Edited By: David Selwood

Impact Factor: 2.507

ISI Journal Citation Reports © Ranking: 2013: 28/58 (Chemistry Medicinal); 173/291 (Biochemistry & Molecular Biology)

Online ISSN: 1747-0285


  1. 1 - 20
  1. Original Articles

    1. Synthesis and anti-inflammatory evaluation of novel C66 analogs for the treatment of LPS-induced acute lung injury

      Jianpeng Feng, Bing Xiao, Wenbo Chen, Ting Ding, Lingfeng Chen, Pengtian Yu, Fengli Xu, Huajie Zhang, Zhiguo Liu and Guang Liang

      Accepted manuscript online: 26 FEB 2015 09:53AM EST | DOI: 10.1111/cbdd.12548

      Thumbnail image of graphical abstract

      Novel asymmetric C66 analogs were synthesized and evaluated their anti-inflammation for the treatment of LPS-induced acute lung injury.

  2. Research Articles

    1. Synthesis and evaluation of 3-(furo[2,3-b]pyridin-3-yl)-4-(1H-indol-3-yl)- maleimides as novel GSK-3β inhibitors and anti-ischemic agents

      Qing Ye, Qiu Li, Yubo Zhou, Lei Xu, Weili Mao, Yuanxue Gao, Chenhui Li, Yuan Xu, Yazhou Xu, Hong Liao, Luyong Zhang, Jianrong Gao, Jia Li and Tao Pang

      Accepted manuscript online: 24 FEB 2015 09:18AM EST | DOI: 10.1111/cbdd.12546

      Thumbnail image of graphical abstract

      A series of novel 3-(furo[2,3-b]pyridin-3-yl)-4-(1H- indol-3- yl)-maleimides were prepared and identified as potent GSK-3β inhibitors and anti-ischemic agents. In the in vivo cerebral ischemia animal model, compound 5o reduced infarct size by 10% and improved the neurological deficit following focal cerebral ischemia.

    2. Combined Molecular Docking, 3D-QSAR, and Pharmacophore Model: Design of Novel Tubulin Polymerization Inhibitors by Binding to Colchicine-binding Site

      Dong-Dong Li, Ya-Juan Qin, Xin Zhang, Yong Yin, Hai-Liang Zhu and Lin-Guo Zhao

      Accepted manuscript online: 24 FEB 2015 09:12AM EST | DOI: 10.1111/cbdd.12545

      Thumbnail image of graphical abstract

      Evaluated by a series of combination of commonly used computer methods such as molecular docking, 3D-QSAR, and pharmacophore model, we can obtain the ultimate 16 tubulin polymerization inhibitors derived from five important basic scaffolds in the field of medicinal chemistry. Among these compounds, compound A-132 with moderate activity in in silico screening was synthesized, and subsequently validated for preliminary inhibition of tubulin polymerization by immunofluorescence assay.

    3. Knockdown of myosin VI inhibits proliferation of hepatocellular carcinoma cells in vitro

      Xiaoming Ma, Jiqi Yan, Wei Chen, Peng Du, Jiaming Xie, Hongpei Yu and Haorong Wu

      Accepted manuscript online: 19 FEB 2015 09:55AM EST | DOI: 10.1111/cbdd.12544

      Thumbnail image of graphical abstract

      1.MYO6 is overexpressed in hepatocellular carcinoma tissues.

      2.Knockdown of MYO6 resulted in a significant diminution in HCC cell proliferation via cell cycle arrest.

      3.Knockdown of MYO6 caused an obvious decrease in PRAS40 phosphorylation and an increase in p38 phosphorylation.

    4. Synthesis and Biological Evaluation of Oxygen-containing Heterocyclic Ring-fused 23-Hydroxybetulinic Acid Derivatives as Antitumor Agents

      Hengyuan Zhang, Fangzheng Li, Peiqing Zhu, Jie Liu, Hequan Yao, Jieyun Jiang, Wencai Ye, Xiaoming Wu and Jinyi Xu

      Accepted manuscript online: 17 FEB 2015 05:01AM EST | DOI: 10.1111/cbdd.12543

      Thumbnail image of graphical abstract

      Most of the newly synthesized compounds exhibited more potent antiproliferative activity than patent compound 23-hydroxybetulinic acid (HBA), especially 13e and 14a were about 4- to 7-fold more potent against all tested cancer cell lines than HBA. Furthermore, the in vivo antitumor activity of 13e and 14a were validated in H22 liver cancer and B16 melanoma xenograft mouse models.

    5. RNAi-mediated silencing of EIF3D alleviates proliferation and migration of glioma U251 and U87MG cells

      Mingliang Ren, Chun Zhou, Hong Liang, Xuhui Wang and Lunshan Xu

      Accepted manuscript online: 13 FEB 2015 06:47AM EST | DOI: 10.1111/cbdd.12542

      Thumbnail image of graphical abstract

      In this study, we found EIF3D expression was positively correlated with WHO grades of gliomas. Knockdown of EIF3D by lentivirus-mediated RNAi caused a significant reduction in growth and migration of glioma cells. EIF3D may serve as a potential therapeutic target in glioma.

  3. Research Letters

    1. Probing the conformational dynamics of the bioactive peptide TLQP 21 in solution: A molecular dynamics study

      Sandipan Chakraborty, Shamim Akhter, Jesús R Requena and Soumalee Basu

      Accepted manuscript online: 12 FEB 2015 09:00AM EST | DOI: 10.1111/cbdd.12541

      Thumbnail image of graphical abstract

      We have explored the folding energy landscape of the peptide TLQP-21 using MD simulation. The peptide is highly flexible in solution and that the region A7-R9 and three C-terminal residues, P19-R21, possess strong helical propensity. The peptide adopts a highly compact globular form stabilized by several hydrogen bonding interactions, π-cationic interactions and strong surface complementarity of hydrophobic residues allows tighter spatial fit of the residues within the core region of the peptide.

  4. Research Articles

    1. Solid-supported synthesis and 5-HT7/5-HT1A receptor affinity of arylpiperazinylbutyl derivatives of 4,5-dihydro-1,2,4-triazine-6-(1H)-one

      Katarzyna Grychowska, Nicolas Masurier, Pascal Verdie, Grzegorz Satała, Andrzej J. Bojarski, Jean Martinez, Maciej Pawłowski, Gilles Subra and Paweł Zajdel

      Accepted manuscript online: 12 FEB 2015 08:59AM EST | DOI: 10.1111/cbdd.12539

      Thumbnail image of graphical abstract

      We have designed and synthesized a novel series of arylpiperazinylbutyl derivatives of 4,5-dihydro-1,2,4-triazine-6(1H)-ones. For this purpose we have developed a new solid-phase methodology enabling construction of the 1,2,4-triazine-6-(1H)-one system from the Fmoc-protected glycine. The study enabled identification of some potent dual 5-HT7/5-HT1A receptor ligands. The structure–affinity relationship analysis revealed that the receptor affinity and selectivity of tested compounds depended on the kind of substituent in position 3 of triazinone fragment as well as substitution pattern of the phenylpiperazine moiety.

    2. 4-Aminoquinoline derivatives as potential antileishmanial agents

      Luciana M. R. Antinarelli, Rafael M. P. Dias, Isabela O. Souza, Wallace P. Lima, Jacy Gameiro, Adilson D. da Silva and Elaine S. Coimbra

      Accepted manuscript online: 12 FEB 2015 08:58AM EST | DOI: 10.1111/cbdd.12540

      Thumbnail image of graphical abstract

      The leishmanicidal activity of a series of 4-aminquinoline (AMQ) derivatives was assayed against Leishmania amazonensis. The compound AMQ-j exhibited a strong leishmanicidal activity its mechanism of action appears to be mediated by mitochondrial dysfunction associated to ROS production.

    3. Synthesis and Evaluation of Cleistanthin-A Derivatives As Potent Vacuolar H+-ATPase Inhibitors

      Yu Zhao, Yapeng Lu, Jinlong Ma and Li Zhu

      Accepted manuscript online: 10 FEB 2015 02:03AM EST | DOI: 10.1111/cbdd.12538

      Thumbnail image of graphical abstract

      Glycosides and alkanes derivatives of Cleistanthin-A have been synthesized. Compounds 3e and 4a displayed strong antiproliferative activity and vacuolar H+-ATPase inhibitory activity.

    4. Novel oxazolidinone antibacterial analogues with a substituted ligustrazine C-ring unit

      Yan Chen, Zhi-Xiong Ruan, Fang Wang, De-Sheng Huangfu, Ping-Hua Sun, Jing Lin and Wei-Min Chen

      Accepted manuscript online: 10 FEB 2015 01:59AM EST | DOI: 10.1111/cbdd.12537

      Thumbnail image of graphical abstract

      A series of novel oxazolidinone derivatives with a substituted ligustrazine C-ring unit were designed and synthesized. Meanwhile, their antibacterial and anti-inflammatory activities were evaluated. Compounds 14a and 14b exhibited both antibacterial and anti-inflammatory potential activities.

    5. Synthesis and antimicrobial evaluation of 6-alkylamino-N–phenyl-pyrazine-2-carboxamides

      Barbora Servusova-Vanaskova, Pavla Paterova, Vladimir Garaj, Jana Mandikova, Jiri Kunes, Lieve Naesens, Petr Jílek, Martin Dolezal and Jan Zitko

      Accepted manuscript online: 10 FEB 2015 01:56AM EST | DOI: 10.1111/cbdd.12536

      Thumbnail image of graphical abstract

      Tuberculosis (TB) belongs to the most dangerous and frequent infection diseases worldwide. Drug-resistant TB-forms as well as increasing number of patient co-infected with HIV constitute a serious problem and emphasize the need for novel drugs. Pyrazinamide, an essential component of short-course anti-TB chemotherapy, was used as a model compound for substances referred in this project. A series of new pyrazinamide derivatives was designed, synthesized and screened for in vitro antimycobacterial activity.

    6. Down-regulation of TPTE2P1 inhibits migration and invasion of gallbladder cancer cells

      Wenjie Lv, Lei Wang, Jianhua Lu, Jiasheng Mu, Yingbin Liu and Ping Dong

      Accepted manuscript online: 10 FEB 2015 01:56AM EST | DOI: 10.1111/cbdd.12533

      Thumbnail image of graphical abstract

      1.Lentivirus-mediated RNAi technique was employed to silence the pseudogene of TPTE2 (TPTE2P1) to enhance the activity of TPTE2.

      2.Depletion of TPTE2P1 remarkably inhibited gallbladder cancer cell migration and invasion.

      3.TPTE2P1 knockdown could elevate the expression of β-catenin via epithelial-mesenchymal transition signaling.

    7. Targeting Influenza A virus RNA Promoter

      Angel Bottini, Surya K. De, Bainan Wu, Changyan Tang, Gabriele Varani and Maurizio Pellecchia

      Accepted manuscript online: 10 FEB 2015 01:56AM EST | DOI: 10.1111/cbdd.12534

      Thumbnail image of graphical abstract

      The influenza A RNA promoter is universally conserved among influenza A virus strains, making it potentially an ideal drug target for novel antiviral agents. Using an NMR-based approach, we report on the characterization and initial SAR studies of RNA binding compounds, including ex vivo anti-influenza activity assays.

  5. Research Letters

    1. New oxidovanadium complexes incorporating thiosemicarbazones and 1, 10-phenanthroline derivatives as DNA cleavager, potential anticancer agents and hydroxyl radical scavenger

      Peng Ying, Pengfei Zeng, Jiazheng Lu, Hongyuan Chen, Xiangwen Liao and Ning Yang

      Accepted manuscript online: 6 FEB 2015 11:00PM EST | DOI: 10.1111/cbdd.12535

      Thumbnail image of graphical abstract

      Four oxidovanadium complexes were synthesized. They exhibited high activity against different cancer cells and low IC50 values in the range 0.2 - 10.0 micro M. In addition, they expressed efficient hydroxyl radical scavenging properties.

  6. Research Articles

    1. Design, synthesis and antimicrobial evaluation of novel quinolone imidazoles and interactions with MRSA DNA

      Ling Zhang, Kannekanti Vijaya Kumar, Rasheed Syed, Rong-Xia Geng and Cheng-He Zhou

      Accepted manuscript online: 2 FEB 2015 02:11AM EST | DOI: 10.1111/cbdd.12532

      Thumbnail image of graphical abstract

      Some compounds exhibited strong anti-MRSA activity with low cytotoxicity. Inducing bacterial resistance by target compounds was much slower than clinical drugs. Interactions of compound and MRSA DNA indicated a possible interaction mechanism.

    2. Discovery of novel 2-(piperidin-4-yl)-1H-benzo[d]imidazole derivatives as potential anti-inflammatory agents

      Qing Li, Qinghua Hu, Xinning Wang, Yang Zong, Leilei Zhao, Junhao Xing, Jinpei Zhou and Huibin Zhang

      Accepted manuscript online: 14 JAN 2015 08:56AM EST | DOI: 10.1111/cbdd.12513

      Thumbnail image of graphical abstract

      Based on the hit compound 5, two series of 2-(piperidin-4-yl)-1H- benzo[d]imidazole derivative 6a-g and 7a-h were designed and synthesized as novel anti-inflammatory agents, in which compound 6e showed most potent inhibitory activity on NO (IC50 = 0.86 μM) and TNF-α (IC50 = 1.87 μM) production.

    3. Discovery of a potent 9-deazaxanthine-Based agent for the Treatment of Obesity-Related Nonalcoholic Fatty Liver Disease

      Jinying Chen, Li Huang, Caifeng Xie, Heying Pei, Liang Ma, Linhong He, Suhong Fu and Lijuan Chen

      Accepted manuscript online: 12 SEP 2014 06:07AM EST | DOI: 10.1111/cbdd.12429

      Thumbnail image of graphical abstract

      Study derivative 8g in two different model to verify its activity for the treatment of obesity –related NAFLD syndrome.

    4. Synthesis and biological evaluation of tricyclic guanidine analogues of batzelladine K for antimalarial, antileishmanial, antibacterial, antifungal and anti-HIV activities

      Nafees Ahmed, Keyur G. Brahmbhatt, Shabana I. Khan, Melissa Jacob, Babu L. Tekwani, Sudeep Sabde, Debashis Mitra, Inder Pal Singh, Ikhlas A. Khan and Kamlesh K. Bhutani

      Accepted manuscript online: 15 JUN 2012 11:37AM EST | DOI: 10.1111/j.1747-0285.2012.01427.x

  7. Research Letters

    1. Virtual and In vitro bioassay screening of phytochemical inhibitors from flavonoids and isoflavones against Xanthine oxidase and Cyclooxygenase-2 for gout treatment

      Yadi Li, Christopher M. Frenz, Zhiwen Li, Mianhua Chen, Yurong Wang, Fengjuan Li, Cheng Luo, Jian Sun, Lars bohlin, Zhenjing Li, Hua Yang and Changlu Wang

      Accepted manuscript online: 3 OCT 2011 03:42PM EST | DOI: 10.1111/j.1747-0285.2011.01248.x


  1. 1 - 20