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Qiu X.-L.,CAS Shanghai Institute of Organic Chemistry | Qiu X.-L.,Wisdom Pharmaceutical Co. | Qing F.-L.,CAS Shanghai Institute of Organic Chemistry | Qing F.-L.,Donghua University
European Journal of Organic Chemistry

Introduction of fluorine atoms or fluorine-containing groups into amino acids has attracted much attention from bioorganic and medicinal chemists because the resulting fluorinated amino acids have found wide application as potential enzyme inhibitors and antitumor (antibacterial) agents. Additionally, it is well known that replacement of naturally occurring amino acid(s) in some peptide chains with their fluorinated counterparts can significantly increase specific protein-ligand or protein-protein interactions, leading to in-creases in the proteolytic and thermal stabilities of peptide compounds and, as a result, promote their therapeutic properties. This microreview summarizes important advances in the synthesis of fluorinated amino acids since 2005. The contents are simply divided into three groups on the basis of amino acid types: fluorinated α-amino acids (F-αAAs), fluorinated β-amino acids (F-βAAs), and fluorinated cyclic amino acids (F-CAAs). © 2011 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim. Source

Zhang K.,Donghua University | Qiu X.-L.,Wisdom Pharmaceutical Co. | Huang Y.,Donghua University | Qing F.-L.,Donghua University | Qing F.-L.,CAS Shanghai Institute of Organic Chemistry
European Journal of Organic Chemistry

An improved method for the efficient copper-mediated trifluoromethylation of terminal alkynes has been developed. This protocol highlights the convenient access to a variety of aryl-substituted trifluoromethylated alkynes by oxidative trifluoromethylation with two equivalents of TMSCF3 at room temperature. Source

Zhu J.,University of California at Irvine | Zhou L.,University of California at Irvine | Wu G.,University of California at Irvine | Konig H.,City of Hope National Medical Center | And 11 more authors.
EMBO Molecular Medicine

RAD51 recombinase activity plays a critical role for cancer cell proliferation and survival, and often contributes to drug-resistance. Abnormally elevated RAD51 function and hyperactive homologous recombination (HR) rates have been found in a panel of cancers, including breast cancer and chronic myeloid leukaemia (CML). Directly targeting RAD51 and attenuating the deregulated RAD51 activity has therefore been proposed as an alternative and supplementary strategy for cancer treatment. Here we show that a newly identified small molecule, IBR2, disrupts RAD51 multimerization, accelerates proteasome-mediated RAD51 protein degradation, reduces ionizing radiation-induced RAD51 foci formation, impairs HR, inhibits cancer cell growth and induces apoptosis. In a murine imatinib-resistant CML model bearing the T315I Bcr-abl mutation, IBR2, but not imatinib, significantly prolonged animal survival. Moreover, IBR2 effectively inhibits the proliferation of CD34+ progenitor cells from CML patients resistant to known BCR-ABL inhibitors. Therefore, small molecule inhibitors of RAD51 may suggest a novel class of broad-spectrum therapeutics for difficult-to-treat cancers. A newly identified RAD51 inhibitor leading to degradation of RAD51 via the proteasome pathway inhibits cancer cell survival and greatly increases life spans in a mouse chronic myeloid leukaemia model. © 2013 The Authors. Published by John Wiley and Sons, Ltd on behalf of EMBO. Source

Luo Y.,University of Sichuan | Zhu Y.,University of Sichuan | Ran K.,University of Sichuan | Liu Z.,University of Sichuan | And 11 more authors.

In this study, a series of novel N-(4-phenylthiazol-2-yl)cinnamamide derivatives (7a-8n) were synthesized and evaluated for their anti-proliferative activities in vitro by MTT assay and a possible antitumor mechanism was also explored. SAR analysis showed that steric effects played an important role on the anti-tumor activity. The most potent analogue 8f showed excellent inhibitions on the K562, Bel7402, A549 and Jurkat cells ranging from sub-micromolar to nanomolar concentration. Compound 8f inhibited Jurkat cells with an IC50 value of 0.035 μM with no apparent toxicity in different non-cancerous cells. Furthermore, it was suggested that the possible mechanism of 8f might be associated with inducing cancer cell apoptosis following flow cytometer analysis and Hoechst 33358 staining assays. © The Royal Society of Chemistry 2015. Source

Li Y.,Wuhan University | Qiu X.,Wisdom Pharmaceutical Co. | Jiang Z.-X.,Wuhan University
Organic Process Research and Development

Even after decades of effort, the efficient synthesis of the structurally simple but highly valuable molecules monodisperse poly(ethylene glycol)s (M-PEGs) remains a long-standing challenge. In this contribution, we give a brief review of the macrocyclic-sulfate-based strategy developed in our lab for the synthesis of M-PEGs and their monofunctionalized derivatives with a focus on the synthetic efficacy and versatility. © 2015 American Chemical Society. Source

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