Abstract:
Chapter 1 describes the general properties of phthalocyanines, synthesis of metallo-
phthalocyanines, their photophysical features and their uses. The concepts of PDT and targeted
therapeutics are also introduced.
Chapter 2 describes the syntheses, characterization, photophysical studies and biological
evaluation of cationic phthalocyanines. The trimethylaminophenoxy substituted phthalocyanines
were synthesized through statistical condensation method, which gave a statistical mixture of
isomers. Di-cationic phthalocyanines were found to be more cytotoxic. The amphiphilicity of the
phthalocyanines played an important role.
Chapter 3 covers the conjugation of phthalocyanines to peptides and is in pursuit of
targeted therapeutics. The conjugation of two peptides, EGFR L1 (six amino acid residues) and
EGFR L2 (twelve amino acid residues), gave conjugates with different charge, length, and
hydrophobicity. The bioconjugates were synthesized via SPS method using typical peptide
coupling agents. Cellular and animal studies are described for the conjugates.
Chapter 4 is a description of the syntheses and characterization of pure regiomeric
phthalocyanines. Previous chapters described, mostly, statistical mixture of Pcs. In this chapter,
strategy to the synthesis of monomeric isomers and their characterization is presented.
Chapter 5 describes the syntheses, characterization and cellular studies of a series of di-
cationic and pegylated phthalocyanines. Statistical condensation was used in the synthesis of
macrocycles. Phthalocyanines with cationic charge at close proximity and on α-substitution
position of the macrocycle were found to be more cytotoxic. In addition, Pc-antibody
bioconjugates are discussed. The biological studies are described for both cationic Pcs and Pc-
conjugates. Just like Chapter 3, this chapter is also in pursuit of targeted therapeutics.
