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

Abstract

A series of porphyrazines (Pzs) with chiral bis-acetal moieties in the β-pyrrole positions ((2,3)-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 . The lead 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. shows marked antitumor effects, 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. 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.

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“…Further looking inside the literature shows that the methylene blue and pentamethincyanin could be also seen as PS materials for PDT processes [8][9][10]. For example, porphyrin and porphyrazine are seen as important PS materials for PDT applications [11][12][13][14]. In the current work, we have studied the photosensitization of metal-free phthalocyanine (Pc) in the original model and its OCH3 (OMe) functionalized derivatives for the purpose of PS applications in PDT.…”