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We report the first exocyclically metallated tetrapyridinoporphyrazine, [tetrakis-(
trans
-Pt(NH
3
)
2
Cl)-tetra(3,4-pyrido)porphyrazine-zinc(
ii
)](NO
3
)
4
(
4
), synthesized in a multistep synthesis starting from 3,4-pyridinedicarbonitrile (
1
). The synthetic procedure involved a platination reaction of the intermediate tetra(3,4-pyrido)porphyrazine-zinc(
ii
) (
2
), whereby the zinc(
ii
) enhanced the solubility of the intermediate enabling the platination reaction. A similar approach to synthesize [tetrakis-(
trans
-Pt(NH
3
)
2
Cl)-tetra(3,4-pyrido)porphyrazine](NO
3
)
4
(
5
) failed due to the unsuitable solubility properties of the intermediate tetra(3,4-pyrido)porphyrazine (
3
). The final product
4
and the intermediates were characterized, the photochemical and photophysical properties were determined and the photocytotoxicities were investigated. We demonstrate that the platinated tetra-pyridinoporphyrazine
4
is a potential photosensitizer for photodynamic therapy (PDT).
Synthesis and biological evaluations of a potential dual chemotherapeutic photosensitizer for photodynamic therapy based on the first exocyclically platinated tetrapyridinoporphyrazine.