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- W2970297839 abstract "7-Fluoro-2-aminophenazine 5,10-dioxide, 1, has displayed in vitro bioreductive selective cytotoxicity, which could acts towards tumors containing hypoxic regions. In this work, we describe some preclinical studies of compound 1 confirming its in vivo antitumor activity. The synthesis of compound 1 was scaled up to 3 g improving the micro-scale yield. Some drug-like properties for compound 1 were theoretically-predicted and others, i. e. aqueous-solubility and toxicity -mutagenicity, in vivo chromosomal-aberrations and ip acute LD50-, were experimentally confirmed. Antitumoral activity was studied in mice bearing hypoxic 4T1-breast-tumor by assessing evolution of the tumor-sizes, animal-survival and bio-chemical/hematological. Compound 1 in vivo efficacy, with the absence of systemic toxicity, was confirmed.. Results highlight the potential of 7-fluoro-2-aminophenazine 5,10-dioxide as promissory therapeutic agent for solid tumors." @default.
- W2970297839 created "2019-09-05" @default.
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- W2970297839 date "2019-08-27" @default.
- W2970297839 modified "2023-10-06" @default.
- W2970297839 title "Selective Hypoxia‐Cytotoxin 7‐Fluoro‐2‐Aminophenazine 5,10‐Dioxide: Toward “Candidate‐to‐Drug” Stage in the Drug‐Development Pipeline" @default.
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- W2970297839 doi "https://doi.org/10.1002/slct.201902601" @default.
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