Chemical and Pharmaceutical Bulletin
Advance online publication
Advance online publication

This service provides final online versions of articles before they are compiled and published in an issue. These versions comprise full-text, peer-reviewed, accepted articles as soon as they are ready for publication, before the release of the compiled print issue, and have DOIs.

Showing 1-3 articles out of 3 articles from Advance online publication
    • |<
    • <
    • 1
    • >
    • >|
  • Kouhei Ishizawa, Hideoki Nagai, Yohei Shimizu, Motomu Kanai
    Article ID: c17-00545
    [Advance publication] Released: August 19, 2017
    JOURNALS PEER REVIEWED FREE ACCESS ADVANCE PUBLICATION

    A catalytic carboxylic acid-selective aldol reaction with trifluoromethyl ketones was developed. Reversible and selective covalent bond formation between a boron catalyst and a carboxylic acid is key to realizing the unprecedented catalytic aldol reaction of simple carboxylic acids. The reaction proceeded chemoselectively at the α-position of carboxylic acid even in the presence of ketone, ester, or amide functional groups in the donor substrates. The chemoselectivity is beneficial for late-stage derivatizations of biologically relevant compounds, as demonstrated by the conversion of indomethacin and triacetylcholic acid.

    View full abstract
    Download PDF (265K)
  • Li Zhang, Zhong-hong Liu, Xun-guan Cheng, Zhu Xia, Yu Liu, Yu Yu
    Article ID: c17-00515
    [Advance publication] Released: August 04, 2017
    JOURNALS PEER REVIEWED FREE ACCESS ADVANCE PUBLICATION

    The application of chemotherapeutics with chemical drugs is always challenged by their high toxicities throughout the body in clinical trials. Here, we reported a smart formulation of docetaxel developed by solid dispersion and effervescent techniques for efficient and safe delivery of chemical drug to lung tissue. To achieve a high delivery to lung with reduced systemic toxicity, docetaxel was loaded into a kind of lecithoid nanoparticles (DTX-LN) which were prepared by a solid dispersion and effervescent method. After intravenous administration of DTX-LN to rabbit, the docetaxel level in lung was approximately 37-fold higher than that of docetaxel injection (DTX-INJ, a commercial injection preparation of DTX/polysorbate 80 micelles) group at 0.5 h and showed the highest tissue distribution among all the organs. Besides, the targeting parameter Re value of AUC0-t ratio (DTX-LN to DTX-INJ) is about 16.69, indicating a significantly enhanced lung targeting ability of DTX-LN. In subacute toxicity study, DTX-LN displayed a reduced hematotoxicity, especially for the negative impacts on white blood cells, lymphocyte and granulocyte when compared with DTX-INJ during both weekly and 3-weekly schedules administration. In addition, histopathological analysis demonstrated that DTX-LN showed less tissue damages on rabbit heart and kidney compared to DTX-INJ. Hence, this work would provide an insight for improving lung delivery efficacy of drugs with reduced systemic toxicity.

    View full abstract
    Download PDF (2302K)
  • Rosa Ma. Chávez-Santos, Paul E. Reyes-Gutiérrez, Rubén O. Torres-Ochoa, Ma. Teresa Ramírez-Apan ...
    Article ID: c17-00409
    [Advance publication] Released: July 22, 2017
    JOURNALS PEER REVIEWED FREE ACCESS ADVANCE PUBLICATION

    In this study, the pyrrolo[2,1-a]isoquinolines 4a-n were synthesized in good yields in a three steps synthesis from the corresponding α,β-unsaturated esters starting materials. These compounds were tested on six human cancer cells lines to measure the cytotoxic activity as a function of the electronic properties and aromaticity of the substituent at the C-2 position of the pyrroloisoquinoline. Our results reveal that the cytotoxic activity could be explained in terms of the distribution of electronic density across the ring joined to C-2. Also, this study identified 3-hydroxy (4d) and 3-chloro (4j) derivatives with powerful cytotoxic activities The IC50 values of these compounds were found to be comparable to those of the commercially available Topotecan, Irinotecan, Etoposide, Tamoxifen, and Cisplatin.

    View full abstract
    Download PDF (899K)
    • |<
    • <
    • 1
    • >
    • >|
feedback
Top