<title>Four-year clinical experience in photodynamic therapy</title>

Abstract

The analysis of the results of photodynamic therapy (PDT) for treatiing malignant neoplasms of skin, breasts, tongue, oral mucose, lower lip, larynx, stomach, bladder, rectum and other locations has been made. During 1992 -1996 years 867 tumoural foci in 222 patients have been treated with PDT. All patients were previously treated with conventional techniques or they were not treated due to contraindications either because of severe accompanying diseases or because of old age. A part of the patients had PDT because of recurrences or intradermal metastases in 1 -2 years after surgical, radial or combined treatment.Up to now we have follow-up control data within 2 months and 4 years. Positive effect of PDT was seen in 93.7% of patients including complete regression of tumours in 64.9% and partial in 28.8%. Currently this new perspective technique of treating malignant neoplasms is successfully being used in Russia; new photosensitizers and light sourses for PDT and fluorecsent tumour diagnostics are being developed as well.

Novel pH-Independent Amphiphilic Chlorophyll a Derivatives with Oligoethyleneglycol Substituents as a Hydrophilic Part: Synthesis and Hydrophilicity Estimation

“…When other structural characteristics are equal the isomeric derivatives with oligoethylene glycol moiety at position 17 have higher chromatographic mobility than derivatives with oligoethylene glycol moiety at position 13(2) (in the case of phorbin derivatives) or at position 15 (in the case of chlorins). For example, the retention time of chlorin e 6 derivatives with oligoethylene glycol moiety at position 17 (27)(28)(29) is approximately 2 min lower than the retention time of analogous derivatives with oligoethylene glycol moiety at position 15 (6)(7)(8). In the case of phorbin derivatives the difference in the retention time for analogous pairs is about 1 min.…”

“…Methyl pheophorbide a 13 (2) diethylene glycol ester (6 Methyl pheophorbide a 13 (2) triethylene glycol ester (7). 73.7 mg (67 %) of compound 7 (13(2)-diastereomers mixture, 13(2)-R/13(2)-S 9:1 according to 1 H NMR) as a dark blue-black crystalline powder was obtained in reaction of 100 mg (0.165 mmol) of 1, 0.5 ml (3.6 mmol) of triethylene glycol, 80.0 mg (0.656 mmol) DMAP and 80.0 mg (0.325 mmol) of 2-chloro-N-methylpyridinium iodide in 5 ml of toluene for 3 hours at full conversion of the starting compound 1.…”

“…Chlorin e 6 13 (1) (25). 36.8 mg (71 %) of compound 25 as a dark blueblack crystalline powder was obtained by the action of 33 % aqueous methylamine solution (1 ml) on the 50 mg (0.062 mmol) of compound 9 in 5 ml of THF for 20 min at complete conversion …”

“…[15][16][17][18] And the influence of the structure of these compounds on the hydrophilicity was not studied systematically. Here we report the synthesis of several phorbines (6)(7)(8)(9)(10)(11)(12)(13)(14)(15)(16)(17)(18)(19)(20)(21) and chlorins (22)(23)(24)(25)(26)(27)(28)(29)(30)(31)(32) with di-, tri-, tetra-, penta-and hexaethylene glycol substituents using methyl pheophorbide a (1) and its derivatives (2)(3)(4)(5) as an initial material (Scheme 1). The influence of the oligoethylene glycol chain length, its position at the macrocycle periphery and the structure of macrocycle on the hydrophilicity of compounds obtained was estimated using their mobility on the reverse phase HPLC data.…”

“…It is known that chlorophyll a derivatives are intensively investigated as photosensitizers (PS) for photodynamic therapy (PDT) in various fields of medicine (oncology, [1][2][3][4][5][6] otolaryngology, [7,8] ophthalmology, [9,10] surgery, [11] treatment of fungal diseases [12] ). Some of them have been already used in clinical practice.…”