Esters of 1,4-benzoxazine and 1,4-benzodioxine compounds 1 and 10, which combine thrombin inhibitory and GPIIb/IIIa antagonistic activity in one molecule are shown to inhibit endothelial cell migration and tube formation in vitro and angiogenesis in the chicken chorioallantoic membrane (CAM) assay. The corresponding carboxylic acids 1 (R-2 = H) and 11 were devoid of anti-angiogenic activity, most probably due to their insufficient entry into the cell. Although thrombin inhibition remains the most probable explanation for their inhibition of angiogenesis, VEGFR2 kinase assay suggest that other targets such as VEGFR2 might be involved. (C) 2012 Elsevier Masson SAS. All rights reserved.
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Yunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R ChinaYunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R China
Zhang, Bing
Huang, Zhi-pu
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Yunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R ChinaYunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R China
Huang, Zhi-pu
Si, Yu
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Yunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R ChinaYunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R China
Si, Yu
Zhang, Ke-tao
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Yunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R ChinaYunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R China
Zhang, Ke-tao
Xu, Xiao-rong
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Yunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R ChinaYunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R China
Xu, Xiao-rong
Chen, Jian-hong
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940 Hosp PLA, Outpatient Dept 1, Lanzhou, Peoples R ChinaYunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R China
Chen, Jian-hong
Zhao, Qing
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Yunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R ChinaYunnan Univ Chinese Med, Coll Basic Med, Coll Chinese Mat Med, Kunming, Yunnan, Peoples R China
Zhao, Qing
Zhang, Xiao-mei
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