Total syntheses of (+)-dictyoceratin-C (1) and (+)-dictyoceratin-A (smenospondiol) (2), hypoxia-selective growth inhibitors isolated from marine sponge, were executed. The absolute stereochemistry of the each compound was determined through the enantioselective total syntheses of them. It revealed that the unnatural enantiomers of them also exhibited the hypoxia-selective growth inhibitory activity against human prostate cancer DU-145 cells.
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http://dx.doi.org/10.1016/j.bmc.2015.01.021 | DOI Listing |
Eur J Med Chem
February 2025
The Affiliated Hospital of Qingdao University, Qingdao University, Qingdao, 266071, China. Electronic address:
Hypoxia is a common feature of various solid tumors, which reduces the sensitivity of tumor cells to both radiotherapy and chemotherapy. However, hypoxia also presents an opportunity for tumor-selective therapy. The prodrug strategy, leveraging the hypoxic nature of the tumor microenvironment, shows significant potential for clinical application.
View Article and Find Full Text PDFMol Pharm
June 2023
Department of Chemical & Materials Engineering, University of Alberta, Edmonton T6G 1H9, Alberta, Canada.
Solid tumors are often poorly vascularized, which impairs oxygen supply and drug delivery to the cells. This often leads to genetic and translational adaptations that promote tumor progression, invasion, metastasis, and resistance to conventional chemo-/radiotherapy and immunotherapy. A hypoxia-directed nanosensitizer formulation of a hypoxia-activated prodrug (HAP) was developed by encapsulating iodoazomycin arabinofuranoside (IAZA), a 2-nitroimidazole nucleoside-based HAP, in a functionally modified carbohydrate-based nanogel, facilitating delivery and accrual selectively in the hypoxic head and neck and prostate cancer cells.
View Article and Find Full Text PDFGastroenterol Rep (Oxf)
August 2022
Department of Surgery and Cancer, Queen Elizabeth the Queen Mother Wing, St Mary's Hospital, Imperial College London, London, UK.
Tumour hypoxia is the inevitable consequence of a tumour's rapid growth and disorganized, inefficient vasculature. The compensatory mechanisms employed by tumours, and indeed the absence of oxygen itself, hinder the ability of all treatment modalities. The clinical consequence is poorer overall survival, disease-free survival, and locoregional control.
View Article and Find Full Text PDFActa Pharm Sin B
March 2022
Department of Pharmaceutics, Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.
The unique characteristics of the tumor microenvironment (TME) could be exploited to develop antitumor nanomedicine strategies. However, in many cases, the actual therapeutic effect is far from reaching our expectations due to the notable tumor heterogeneity. Given the amplified characteristics of TME regulated by vascular disrupting agents (VDAs), nanomedicines may achieve unexpected improved efficacy.
View Article and Find Full Text PDFRedox Biol
June 2022
Department of Oncology, University of Alberta, Edmonton, Alberta, AB T6G 2R3, Canada. Electronic address:
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