2. Academic Validation
  3. Discovery of the Antitumor Effects of a Porphyrazine Diol (Pz 285) in MDA-MB-231 Breast Tumor Xenograft Models in Mice

Discovery of the Antitumor Effects of a Porphyrazine Diol (Pz 285) in MDA-MB-231 Breast Tumor Xenograft Models in Mice

  • ACS Med Chem Lett. 2017 Jun 29;8(7):705-709. doi: 10.1021/acsmedchemlett.7b00063.
Irawati K Kandela 1,  Katherine J McAuliffe 2,  Lauren E Cochran 2,  Anthony G M Barrett 3,  Brian M Hoffman 4,  Andrew P Mazar 1,  Evan R Trivedi 2
Affiliations

Affiliations

  • 1 Center for Developmental Therapeutics, Chemistry of Life Processes Institute, Northwestern University, Evanston, Illinois 60208, United States.
  • 2 Department of Chemistry, Oakland University, Rochester, Michigan 48309, United States.
  • 3 Department of Chemistry, Imperial College of Science, Technology, and Medicine, London SW7 2AZ, England.
  • 4 Departments of Chemistry and Molecular Biosciences, Northwestern University, Evanston, Illinois 60208, United States.
PMID: 28740602 DOI: 10.1021/acsmedchemlett.7b00063
Abstract

A series of porphyrazines (Pzs) with chiral bis-acetal moieties in the β-pyrrole positions ((2R,3R)-2,3-dimethyl-2,3-dimethoxy-1,4-diox-2-ene) have been synthesized and screened as antitumor agents in MDA-MB-231 breast tumor cells in vitro. The lead Pz 285 was further tested in a mouse tumor xenograft model with Td-tomato-luc2 fluorescent breast tumor cells (MDA-MB-231 LM24 Her2+) that are highly metastatic to the lungs. Pz 285 shows marked antitumor effects in vivo, with treated mice exhibiting longer median survival that we attribute to smaller primary tumor regrowth after resection and less occurrence of metastasis when compared to vehicle control groups. Pz 285 is further compared to the clinically approved chemotherapeutic doxorubicin (Dox). This report lays the groundwork for development of an understudied class of compounds for classical chemotherapy.

Keywords

MDA-MB-231 LM24 Her2+; Porphyrazine; antitumor.

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