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• W2466330278 abstract "// Ping Song 2, * , Xin Yao 1, 2, * , Ting Zhong 1, 2 , Shuang Zhang 1, 2 , Yang Guo 1, 2 , Wei Ren 1, 2 , Dan Huang 1, 2 , Xiao-Chuan Duan 1, 2 , Yi-Fan Yin 1 , Shu-Shi Zhang 1 , Xuan Zhang 1, 2 1 Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China 2 Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China * These authors have contributed equally to this work Correspondence to: Xuan Zhang, email: xuanzhang@bjmu.edu.cn Keywords: paclitaxel, 3-(2-Nitrophenyl) propionic acid, bioreductive prodrug, tumor hypoxia, anti-tumor efficacy Received: February 15, 2016     Accepted: June 09, 2016     Published: June 27, 2016 ABSTRACT Hypoxia is an important microenvironmental pressure present in the majority of solid tumors and, so, tumor hypoxia might be considered an attractive target for tumor therapy. One strategy for targeting hypoxia is to develop bioreductive prodrugs. In the present research, we synthesized a bioreductive paclitaxel prodrug, 3-(2-Nitrophenyl) propionic acid-paclitaxel (NPPA-PTX). The stability of NPPA-PTX in PBS and rat plasma was investigated. The anti-tumor activity of NPPA-PTX was also evaluated in vitro and in vivo . The results of our stability study indicated that NPPA-PTX was stable in PBS and rat plasma as well as in the blood circulation. The in vitro and in vivo anti-tumor activity of NPPA-PTX was confirmed in both KB cells and MDA-MB-231 cells. Our results also indicated that NPPA-PTX could completely convert to active PTX in tumor tissues and produced the anti-tumor activity in both KB and MDA-MB-231 tumor-bearing nude mice. We suggest that the dissociated PTX which converted from NPPA-PTX in tumor tissues played a key role in producing anti-tumor activity. Considering all our results, we suggest that NPPA-PTX is a novel bioreductive PTX prodrug which could undergo further evaluation." @default.
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• W2466330278 date "2016-06-27" @default.
• W2466330278 modified "2023-09-25" @default.
• W2466330278 title "The anti-tumor efficacy of 3-(2-Nitrophenyl) propionic acid-paclitaxel (NPPA-PTX): a novel paclitaxel bioreductive prodrug" @default.
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• W2466330278 doi "https://doi.org/10.18632/oncotarget.10310" @default.
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