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  3. Synthesis and evaluation of new dinitrobenzamide mustards in human prostate cancer

Synthesis and evaluation of new dinitrobenzamide mustards in human prostate cancer

  • Bioorg Med Chem Lett. 2021 Jan 1:31:127697. doi: 10.1016/j.bmcl.2020.127697.
Alireza Basiri 1,  Wenting Zhang 1,  Jered Garrison 2
Affiliations

Affiliations

  • 1 Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, 985830 Nebraska Medical Center, Omaha, NE 68198, United States; Center for Drug Delivery and Nanomedicine, University of Nebraska Medical Center, 985830 Nebraska Medical Center, Omaha, NE 68198, United States.
  • 2 Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, 985830 Nebraska Medical Center, Omaha, NE 68198, United States; Department of Biochemistry and Molecular Biology, College of Medicine, University of Nebraska Medical Center, 985870 Nebraska Medical Center, Omaha, NE 68198, United States; Center for Drug Delivery and Nanomedicine, University of Nebraska Medical Center, 985830 Nebraska Medical Center, Omaha, NE 68198, United States; Eppley Cancer Center, University of Nebraska Medical Center, 985950 Nebraska Medical Center, Omaha, NE 68198, United States. Electronic address: jcgarrison@unmc.edu.
PMID: 33220402 DOI: 10.1016/j.bmcl.2020.127697
Abstract

Tumor hypoxia has been widely explored over the years as a diagnostic and therapeutic marker. Herein, we have reported the design and synthesis of a series of dinitrobenzamide mustards (DNBM) based on the PR-104A hypoxia-selective prodrug. Specifically, we explored the impact of various leaving groups and the introduction of a carboxylic acid group on the biological performance of the DNBM constructs. Once in hand, the Log D values, cytotoxicity in PC-3 and DU-145 human prostate Cancer cells lines and the hypoxia selectivities of the DNBM analogs were examined. Overall, the DNBM constructs were found to be tolerant to modifications with none of the explored modifications substantially degrading the cytotoxic potential of the constructs.

Keywords

DNBM; Hypoxia; Prodrug; Prostate cancer.

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