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Novel 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine fused chlorins as very active photodynamic agents for melanoma cells.

Abstract
The development of new stable 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine-fused chlorins with high absorption properties at 650 nm, and their impressive photosensitizer ability against melanotic and amelanotic cancer cells is described. Comparison between a diester-substituted chlorin with the corresponding dihydroxymethyl derivative demonstrated that the increased hydrophilicity of the latter is crucial to ensure nanomolar activity against melanoma cells. The new photosensitizer leads to death of human melanoma cells being both apoptosis and necrosis in equal parts involved in the treatment response. The dihydroxymethyl-chlorin was particularly active against human melanocytic melanoma A375 cells, which can be viewed as a solution to overcome the resistance of melanotic melanoma to photodynamic therapy.
AuthorsNelson A M Pereira, Mafalda Laranjo, Marta Pineiro, Arménio C Serra, Kathleen Santos, Ricardo Teixo, Ana Margarida Abrantes, Ana Cristina Gonçalves, Ana Bela Sarmento Ribeiro, João Casalta-Lopes, M Filomena Botelho, Teresa M V D Pinho e Melo
JournalEuropean journal of medicinal chemistry (Eur J Med Chem) Vol. 103 Pg. 374-80 (Oct 20 2015) ISSN: 1768-3254 [Electronic] France
PMID26383124 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2015 Elsevier Masson SAS. All rights reserved.
Chemical References
  • Antineoplastic Agents
  • Photosensitizing Agents
  • Porphyrins
  • Pyrazoles
Topics
  • Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
  • Apoptosis (drug effects)
  • Cell Line, Tumor
  • Cell Proliferation (drug effects)
  • Dose-Response Relationship, Drug
  • Drug Screening Assays, Antitumor
  • Humans
  • Melanoma (drug therapy, pathology)
  • Molecular Structure
  • Photochemotherapy
  • Photosensitizing Agents (chemical synthesis, chemistry, pharmacology)
  • Porphyrins (chemical synthesis, chemistry, pharmacology)
  • Pyrazoles (chemical synthesis, chemistry, pharmacology)
  • Structure-Activity Relationship

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