Chemical Biology & Drug Design

Cover image for Vol. 83 Issue 3

March 2014

Volume 83, Issue 3

Pages i–iii, 259–378

  1. Issue Information

    1. Top of page
    2. Issue Information
    3. Research Letters
    4. Research Articles
    5. Research Letter
    1. Issue Information (pages i–iii)

      Version of Record online: 25 FEB 2014 | DOI: 10.1111/cbdd.12214

  2. Research Letters

    1. Top of page
    2. Issue Information
    3. Research Letters
    4. Research Articles
    5. Research Letter
    1. Ablation of Breast Cancer Cells Using Trastuzumab-Functionalized Multi-Walled Carbon Nanotubes and Trastuzumab-Diphtheria Toxin Conjugate (pages 259–265)

      Mojtaba Oraki Kohshour, Sako Mirzaie, Majid Zeinali, Mansour Amin, Mohammad Said Hakhamaneshi, Ali Jalili, Nader Mosaveri and Mostafa Jamalan

      Version of Record online: 26 DEC 2013 | DOI: 10.1111/cbdd.12244

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      Trastuzumab (Herceptin®) was directly conjugated to diphtheria toxin (DT). Also, covalent conjugates of trastuzumab and multiwalled carbon nanotubes (MWCNT) were constructed. The prepared constructs were used to ablate HER2-overexpressing SK-BR-3 cancer cell line. Targeting of MWCNTs to cancerous cells using trastuzumab followed by exposure of cells to near-infrared (NIR) radiation was more efficient in repression of cell proliferation than treatment for cancer cells with trastuzumab-DT. Our results also showed that conjugation linkers can significantly affect the cytotoxicity of MWCNT-immunoconjugates.

    2. The High-Affinity Maltose Switch MBP317-347 has Low Affinity for Glucose: Implications for Targeting Tumors with Metabolically Directed Enzyme Prodrug Therapy (pages 266–271)

      Gilmer Valdes, Reinhard W. Schulte, Marc Ostermeier and Keisuke S. Iwamoto

      Version of Record online: 26 DEC 2013 | DOI: 10.1111/cbdd.12249

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      We show the potential for exploiting the Warburg Effect, which sets apart aggressive tumors from normal tissues, to target the high glucose requirement and the resultant high lactate content of tumors compared to most normal tissues. We present proof of concept using a low-affinity molecular protein switch that is activated past a threshold of millimolar glucose (as a model for lactate, the ideal substrate) concentrations. Once activated only within the tumor, a prodrug would be converted into a drug.

  3. Research Articles

    1. Top of page
    2. Issue Information
    3. Research Letters
    4. Research Articles
    5. Research Letter
    1. Effectiveness of Novel 5-(5-amino-1-aryl-1H-pyrazol-4-yl)-1H-tetrazole Derivatives Against Promastigotes and Amastigotes of Leishmania amazonensis (pages 272–277)

      Viviane dos Santos Faiões, Leonor L. Leon, Marilene M. Canto-Cavalheiro, Eduardo C. Torres-Santos, Alice M. R. Bernardino, Percilene F. Vegi and Maurício S. dos Santos

      Version of Record online: 30 OCT 2013 | DOI: 10.1111/cbdd.12235

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      A series of substituted 5-(5-amino-1-aryl-1H-pyrazol-4-yl)-1H-tetrazoles were synthesized and evaluated for in vitro antileishmanial activity. The cytotoxicity of these compounds was evaluated on murine cells, giving access to the corresponding selectivity index (SI).

    2. Antimicrobial Activity and SAR Study of New Gemini Imidazolium-Based Chlorides (pages 278–288)

      Łukasz Pałkowski, Jerzy Błaszczyński, Andrzej Skrzypczak, Jan Błaszczak, Karolina Kozakowska, Joanna Wróblewska, Sylwia Kożuszko, Eugenia Gospodarek, Jerzy Krysiński and Roman Słowiński

      Version of Record online: 26 DEC 2013 | DOI: 10.1111/cbdd.12236

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      A series of new 3,3′-(α,ω-dioxaalkan)bis(1-alkylimidazolium) chlorides were synthesized. They were characterized with respect to surface active properties and antimicrobial activity. Dominance-based Rough Set Approach (DRSA) was then used to analyze relationships between structure, surface properties and antimicrobial activity.

    3. Discovery of Synthetic Leishmania Inhibitors by Screening of a 2-Arylbenzothiophene Library (pages 289–296)

      Vivian I. Bonano, Jenicer K. U. Yokoyama-Yasunaka, Danilo C. Miguel, Scott A. Jones, Jeffrey A. Dodge and Silvia R. B. Uliana

      Version of Record online: 26 DEC 2013 | DOI: 10.1111/cbdd.12239

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      The screening of an estrogen receptor modulator related library of compounds allowed the identification of benzothiophenes as a new scaffold with antileishmanial properties. Three compounds devoid of estrogen receptor interaction were identified with increased potency against the parasite. Structure-activity data for the synthetic benzothiophenes evaluated in this study indicates that optimal antileishmanial potency is dependent on the presence of two basic side chains.

    4. Synthesis and Evaluation of Novel Oleanolic Acid Derivatives as Potential Antidiabetic Agents (pages 297–305)

      Liying Zhang, Xiaojian Jia, Jizhe Dong, Dongyin Chen, Jun Liu, Luyong Zhang and Xiaoan Wen

      Version of Record online: 1 FEB 2014 | DOI: 10.1111/cbdd.12241

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      A series of oleanolic acid derivatives were designed and synthesized in order to search for antidiabetic agents that inhibit hepatic glucose production and promote hepatic glucose consumption simultaneously. All of the compounds were evaluated biologically in vitro using glycogen phosphorylase and HepG2 cells. Compound 8g exhibited the best activity in inhibiting glycogen phosphorylase, and satisfactory activity in promoting glucose consumption.

    5. Design, Synthesis and Biological Evaluation of Pazopanib Derivatives as Antitumor Agents (pages 306–316)

      Yuping Jia, Jian Zhang, Jinhong Feng, Fuming Xu, Huili Pan and Wenfang Xu

      Version of Record online: 1 FEB 2014 | DOI: 10.1111/cbdd.12243

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      A series of novel Pazopanib derivatives, were designed and synthesized as anticancer agents. Compounds P2d and P2e demonstrated outstanding inhibitory activity against VEGFR-2(IC50 = 0.025 μm, IC50 = 0.012 μm) and ABL1 (IC50 = 0.062 μm, IC50 = 0.022 μm), and higher anti-angiogenic activity (0.001 μm, 0.001 μm) compared with Pazopanib (IC50 = 0.043 μm, IC50 = 0.62 μm, 0.01 μm).

    6. Effect of HA14-1 on Apoptosis-Regulating Proteins in HeLa Cells (pages 317–323)

      Kanwal Rehman, Muhammad Tariq, Muhammad S. H. Akash, Zeeshan Gillani and Mehmood H. Qazi

      Version of Record online: 26 DEC 2013 | DOI: 10.1111/cbdd.12245

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      The structure of four proteins (Bcl-2, Bcl-xl, Bax, and Bak) was acquired to check the binding effect of HA14-1. HA14-1 showed the ability to occupy the putative hydrophobic pocket of Bcl-2 and Bcl-xl protein only. HA14-1 may provoke apoptotic pathway in HeLa cells by targeting Bcl-2 proteins.

    7. Design, Synthesis, and Biological Evaluation of Andrographolide Derivatives as Potent Hepatoprotective Agents (pages 324–333)

      Chunlei Tang, Guolong Gu, Bin Wang, Xin Deng, Xiaoyun Zhu, Hai Qian and Wenlong Huang

      Version of Record online: 26 DEC 2013 | DOI: 10.1111/cbdd.12246

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      Aqueous solubility improved andrographolide derivatives were designed, synthesized, characterized, and evaluated for in vivo hepatoprotective activity against CCl4-induced liver injury in mice. The most promising compound 9d significantly improved liver enzyme (ALT and AST) activity, with high potency to be a new lead.

    8. Synthesis and Biological Evaluation of Heterocyclic Carboxylic Acyl Shikonin Derivatives (pages 334–343)

      Xiao-Ming Wang, Hong-Yan Lin, Wen-Yao Kong, Jing Guo, Jing Shi, Shou-Cheng Huang, Jin-Liang Qi, Rong-Wu Yang, Hong-Wei Gu and Yong-Hua Yang

      Version of Record online: 26 DEC 2013 | DOI: 10.1111/cbdd.12247

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      A series of shikonin derivatives which were acylated selectively by various thiophene or indol carboxylic acids at the side chain of shikonin were synthesized and their biological activities were also evaluated as potential tubulin inhibitors. Among them, compound 3 and compound 8 exhibited good antiproliferative activity of A875 and HeLa cancer cell lines in vitro. The docking results demonstrated that compound 3 bound nicely with the active site of tubulin.

    9. Synthesis of Isosteric Triterpenoid Derivatives and Antifungal Activity (pages 344–349)

      Adrine Innocente, Bruna B. Casanova, Fernanda Klein, Aline D. Lana, Dariane Pereira, Mauro N. Muniz, Pascal Sonnet, Grace Gosmann, Alexandre M. Fuentefria and Simone C. B. Gnoatto

      Version of Record online: 1 FEB 2014 | DOI: 10.1111/cbdd.12251

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      Six compounds were synthesised and tested against eleven mucocutaneous and cutaneous mycotic agents. Two active compounds were identified. The MIC values of the derivatives of ursolic and betulinic acids were in the range of 16–32 µg/mL and 4–16 µg/mL, respectively, whereas fungicidal effects were observed at concentrations ranging from 16 to 128 µg/mL and 8 to 128 µg/mL, respectively.

    10. Biological Activity of Sporolides A and B from Salinispora tropica: in silico Target Prediction Using Ligand-Based Pharmacophore Mapping and in vitro activity Validation on HIV-1 Reverse Transcriptase (pages 350–361)

      Kesavan Dineshkumar, Vasudevan Aparna, Kantilal Z. Madhuri and Waheeta Hopper

      Version of Record online: 1 FEB 2014 | DOI: 10.1111/cbdd.12252

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      Sporolides are unique and novel structure from Salinispora tropica, it possess no biological activity that makes them interesting candidates for targeting diverse biological activities. Biological target prediction of sporolides was carried out using Ligand-based pharmacophore screening. New biological activity predicted for sporolides are HIV-1 reverse transcriptase. Sporolides exhibited inhibitory activity against HIV-1 reverse transcriptase in in vitro fluorescent assay.

    11. Design of 99mTc-DTPA-CLP and Preliminary Evaluation in Rats (pages 362–366)

      Burcu Altıparmak, Fatma Y. Lambrecht and Ozge Er

      Version of Record online: 1 FEB 2014 | DOI: 10.1111/cbdd.12253

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      The current study demonstrated that DTPA-CLP is labeled with 99mTc with high yield. 99mTc-DTPA-CLP remained stable in serum. The radiolabeled peptide conjugate has greater affinity to those cells expressing matrix metalloproteinase inhibitor as indicated by its accumulation in organs such as uterus, ovary, liver and breast.

  4. Research Letter

    1. Top of page
    2. Issue Information
    3. Research Letters
    4. Research Articles
    5. Research Letter
    1. Unsymmetrical Oxovanadium Complexes Derived from Salicylaldehyde and Phenanthroline: Synthesis, DNA Interactions, and Antitumor Activities (pages 367–378)

      Xiangwen Liao, Weijian Pan, Rongwei He, Haiwei Guo, Peng Ying and Jiazheng Lu

      Version of Record online: 26 DEC 2013 | DOI: 10.1111/cbdd.12248

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      Two unsymmetrical oxovanadium complexes were synthesized. They can efficiently cleave plasmid DNA and exhibit high cytotoxic activities against tumor cells with lower IC50 values.

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