title: Novel hypoxia-targeting Pt(iv) prodrugs.
abstract: Novel Pt(iv) prodrugs targeting hypoxia inducible factor HIF-1α were prepared for evaluating their antitumor activity on hypoxic cancer cells for the first time. The resulting Pt(iv) prodrug exhibited effective inhibition on tumor growth in the HCT-116 xenograft mouse model with low toxicity in vivo.
authors.affiliation: Pharmaceutical Research Center and School of Chemistry and Chemical Engineering, Jiangsu Province Hi-Tech Key Laboratory for Biomedical Research, Southeast University, Nanjing 211189, P. R. China. sgou@seu.edu.cn.
authors.forename: Zichen
authors.identifier: http://orcid.org/0000-0002-6469-7869
authors.initials: Z
authors.lastname: Xu
authors.affiliation: Pharmaceutical Research Center and School of Chemistry and Chemical Engineering, Jiangsu Province Hi-Tech Key Laboratory for Biomedical Research, Southeast University, Nanjing 211189, P. R. China. sgou@seu.edu.cn.
authors.forename: Jian
authors.initials: J
authors.lastname: Zhao
authors.affiliation: Pharmaceutical Research Center and School of Chemistry and Chemical Engineering, Jiangsu Province Hi-Tech Key Laboratory for Biomedical Research, Southeast University, Nanjing 211189, P. R. China. sgou@seu.edu.cn.
authors.forename: Shaohua
authors.identifier: http://orcid.org/0000-0001-5216-3838
authors.initials: S
authors.lastname: Gou
authors.affiliation: Pharmaceutical Research Center and School of Chemistry and Chemical Engineering, Jiangsu Province Hi-Tech Key Laboratory for Biomedical Research, Southeast University, Nanjing 211189, P. R. China. sgou@seu.edu.cn.
authors.forename: Gang
authors.initials: G
authors.lastname: Xu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D015687:Cell Hypoxia / Q000187:drug effects*; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D045325:HCT116 Cells; D006801:Humans; D051795:Hypoxia-Inducible Factor 1, alpha Subunit / Q000037:antagonists & inhibitors*; D051379:Mice; D015394:Molecular Structure; D009944:Organoplatinum Compounds / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D011355:Prodrugs / Q000009:adverse effects / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; C497442:HIF1A protein, human; D051795:Hypoxia-Inducible Factor 1, alpha Subunit; D009944:Organoplatinum Compounds; D011355:Prodrugs