Synthesis of fluorine analogues of protoporphyrin potentially useful for diagnosis and therapy of tumors.
- 1 January 1990
- journal article
- research article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 38 (8) , 2175-2178
- https://doi.org/10.1248/cpb.38.2175
Abstract
With the aim of obtaining a porphyrin derivative useful for diagnosis and therapy of cancer, fluorine analogues of protoporphyrin, in which the vinyl group(s) were replaced by difluorovinyl group(s), were synthesized by the reaction of the formylporphyrins with sodium chlorodifluoroacetate in the presence of triphenylphosphine. Some improvements in the reported procedures for the synthesis of formylporphyrins are also described. Preliminary results of biological tests of the products showed that 82, 82-difluoroprotoporphyrin accumulates to gastric cancer more selectively than other fluorine analogues and that 32, 32, 82, 82-tetrafluoroprotoporphyrin is taken up by rat hepatoma cells more readily than the others.Keywords
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