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European journal of medicinal chemistry 163건

  1. [해외논문]   Thieno[2,3-b]pyridine derivatives are potent anti-platelet drugs, inhibiting platelet activation, aggregation and showing synergy with aspirin   SCI SCIE

    Binsaleh, Naif K. (School of Healthcare Science, Manchester Metropolitan University, Manchester M1 5GD, UK ) , Wigley, Catherine A. (School of Healthcare Science, Manchester Metropolitan University, Manchester M1 5GD, UK ) , Whitehead, Kathryn A. (School of Healthcare Science, Manchester Metropolitan University, Manchester M1 5GD, UK ) , van Rensburg, Michelle (School of Chemical Sciences, The University of Auckland, New Zealand ) , Reynisson, Johannes (School of Chemical Sciences, The University of Auckland, New Zealand ) , Pilkington, Lisa I. (School of Chemical Sciences, The University of Auckland, New Zealand ) , Barker, David (School of Chemical Sciences, The University of Auckland, New Zealand ) , Jones, Sarah (School of Healthcare Science, Manchester Metropolitan University, Manchester M1 5GD, UK ) , Dempsey-Hibbert, Nina C. (School of Healthcare Science, Manchester Metropolitan University, Manchester M1 5GD, UK)
    European journal of medicinal chemistry v.143 ,pp. 1997 - 2004 , 2018 , 0223-5234 ,

    초록

    Abstract Drugs which inhibit platelet function are commonly used to prevent blood clot formation in patients with Acute Coronary Syndromes (ACS) or those at risk of stroke. The thieno[3,2- c ]pyridine class of therapeutic agents, of which clopidogrel is the most commonly used, target the P2Y 12 receptor, and are often used in combination with acetylsalicylic acid (ASA). Six thieno[2,3- b ]pyridine were assessed for in vitro anti-platelet activity; all derivatives showed effects on both platelet activation and aggregation, and showed synergy with ASA. Some compounds demonstrated greater activity when compared to clopidogrel. These compounds, therefore, represent potential novel P2Y 12 inhibitors for improved treatment for patients. Highlights Thieno[2,3- b ]pyridines inhibited platelet activation and aggregation. Thieno[2,3- b ]pyridines showed synergy with aspirin. Tested compounds had greater activity to clinically used thieno[3,2- c ]pyridines. Thieno[2,3- b ]pyridines have been found to be a novel class of P2Y 12 inhibitors. Graphical abstract [DISPLAY OMISSION]

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    회원님의 원문열람 권한에 따라 열람이 불가능 할 수 있으며 권한이 없는 경우 해당 사이트의 정책에 따라 회원가입 및 유료구매가 필요할 수 있습니다.이동하는 사이트에서의 모든 정보이용은 NDSL과 무관합니다.

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  2. [해외논문]   Camptothecin-psammaplin A hybrids as topoisomerase I and HDAC dual-action inhibitors   SCI SCIE

    Cincinelli, Raffaella (Department of Food, Environmental and Nutritional Sciences, Division of Chemistry and Molecular Biology, Università) , Musso, Loana (degli Studi di Milano, via Celoria 2, 20133 Milan, Italy ) , Artali, Roberto (Department of Food, Environmental and Nutritional Sciences, Division of Chemistry and Molecular Biology, Università) , Guglielmi, Mario (degli Studi di Milano, via Celoria 2, 20133 Milan, Italy ) , Bianchino, Erminia (Scientia Advice, di Roberto Artali, 20832 Desio, MB, Italy ) , Cardile, Francesco (Biogem, Research Institute, Ariano Irpino, AV, Italy ) , Colelli, Fabiana (Biogem, Research Institute, Ariano Irpino, AV, Italy ) , Pisano, Claudio (Biogem, Research Institute, Ariano Irpino, AV, Italy ) , Dallavalle, Sabrina (Biogem, Research Institute, Ariano Irpino, AV, Italy )
    European journal of medicinal chemistry v.143 ,pp. 2005 - 2014 , 2018 , 0223-5234 ,

    초록

    Abstract Recent studies have demonstrated enhanced anticancer effects of combination therapy consisting of camptothecin derivatives and HDAC inhibitors. To exploit this synergy in a single active compound, we designed new dual-acting multivalent molecules simultaneously targeting topoisomerase I and HDAC. In particular, a selected compound containing a camptothecin and the psammaplin A scaffold showed a broad spectrum of antiproliferative activity, with IC 50 values in the nanomolar range. Preliminary in vivo results indicated a strong antitumor activity on human mesothelioma primary cell line MM473 orthotopically xenografted in CD-1 nude mice and very high tolerability. Highlights A new dual HDAC-topoisomerase I inhibitor was investigated. Molecular docking was used to predict the optimal conformation in Top1/HDAC sites. The compound showed antiproliferative activity with IC 50 values in the nanamolar range. The compound exhibited an appreciable in vivo antitumor activity. Graphical abstract [DISPLAY OMISSION]

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    회원님의 원문열람 권한에 따라 열람이 불가능 할 수 있으며 권한이 없는 경우 해당 사이트의 정책에 따라 회원가입 및 유료구매가 필요할 수 있습니다.이동하는 사이트에서의 모든 정보이용은 NDSL과 무관합니다.

    NDSL에서는 해당 원문을 복사서비스하고 있습니다. 아래의 원문복사신청 또는 장바구니담기를 통하여 원문복사서비스 이용이 가능합니다.

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  3. [해외논문]   Corrigendum to “Blockade of STAT3 activation by sorafenib derivatives through enhancing SHP-1 phosphatase activity” [Eur. J. Med. Chem. 55 (2012) 220–227]   SCI SCIE

    Chen, Kuen-Feng (Department of Medical Research, National Taiwan University Hospital, Taipei, Taiwan ) , Tai, Wei-Tien (National Center of Excellence for Clinical Trial and Research, National Taiwan University Hospital, Taipei, Taiwan ) , Hsu, Cheng-Yi (Institute of Biopharmaceutical Sciences, National Yang-Ming University, Taipei, Taiwan ) , Huang, Jui-Wen (Biomedical Engineering Research Laboratories, Industrial Technology Research Institute, Hsinchu, Taiwan ) , Liu, Chun-Yu (Institute of Biopharmaceutical Sciences, National Yang-Ming University, Taipei, Taiwan ) , Chen, Pei-Jer (Department of Medical Research, National Taiwan University Hospital, Taipei, Taiwan ) , Kim, InKi (ASAN Institute for Life Science, ASAN Medical Center, Seoul, Republic of Korea ) , Shiau, Chung-Wai (Institute of Biopharmaceutical Sciences, National Yang-Ming University, Taipei, Taiwan)
    European journal of medicinal chemistry v.143 ,pp. 2015 - 2015 , 2018 , 0223-5234 ,

    초록

    Abstract Recent studies have demonstrated enhanced anticancer effects of combination therapy consisting of camptothecin derivatives and HDAC inhibitors. To exploit this synergy in a single active compound, we designed new dual-acting multivalent molecules simultaneously targeting topoisomerase I and HDAC. In particular, a selected compound containing a camptothecin and the psammaplin A scaffold showed a broad spectrum of antiproliferative activity, with IC 50 values in the nanomolar range. Preliminary in vivo results indicated a strong antitumor activity on human mesothelioma primary cell line MM473 orthotopically xenografted in CD-1 nude mice and very high tolerability. Highlights A new dual HDAC-topoisomerase I inhibitor was investigated. Molecular docking was used to predict the optimal conformation in Top1/HDAC sites. The compound showed antiproliferative activity with IC 50 values in the nanamolar range. The compound exhibited an appreciable in vivo antitumor activity. Graphical abstract [DISPLAY OMISSION]

    원문보기

    원문보기
    무료다운로드 유료다운로드

    회원님의 원문열람 권한에 따라 열람이 불가능 할 수 있으며 권한이 없는 경우 해당 사이트의 정책에 따라 회원가입 및 유료구매가 필요할 수 있습니다.이동하는 사이트에서의 모든 정보이용은 NDSL과 무관합니다.

    NDSL에서는 해당 원문을 복사서비스하고 있습니다. 아래의 원문복사신청 또는 장바구니담기를 통하여 원문복사서비스 이용이 가능합니다.

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