- Synthesis and evaluation of new 5-aminolevulinic acid derivatives as prodrugs of protoporphyrin for photodynamic therapy
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Protoporphyrin IX (PpIX) is used as a photosensitizer in the photodynamic diagnosis (PDD) and photodynamic therapy (PDT) of cancer and is synthesized intracellularly from 5-aminolevulinic acid (5-ALA) precursors. Thirteen novel 5-ALA derivatives were designed and synthesized appropriately with tailored hydrophilicity and lipophilicity. The generation of PpIX was detected and their antitumor activity in vitro and in vivo was also investigated. It was shown that compounds 9b-c, 11b-c and 13a displayed a characteristic long wavelength absorption peak at 593 nm after 5 h incubation in mice fibrosarcoma S180 cells. After being exposed to 600 nm laser light irradiation, these compounds can inhibit cell proliferation in S180 cells in vitro. The growth of S180 cell tumors in Kunming mice was significantly inhibited by these compounds in vivo. Among these compounds, 13a has low dark toxicity and high phototoxicity, which makes it an effective and promising prodrug for PDT.
- Zhu, Wei,Gao, Ying-Hua,Song, Chun-Hong,Lu, Zhi-Bin,Namulinda, Tabbisa,Han, Yi-Ping,Yan, Yi-Jia,Wang, Lai-Xing,Chen, Zhi-Long
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p. 1623 - 1630
(2017/11/16)
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- 5-[(PIPERAZIN-1-YL)-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS INHIBITORS FOR THE TREATMENT OF OSTEOARTHRITIS
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The present invention discloses compounds according to Formula (I), wherein R, R2, R3a, R3b, and Cy are as defined herein. The present invention discloses compounds inhibiting ADAMTS, methods for their production, pharmaceutical compositions comprising the same and methods for the prophylaxis and/or treatment of inflammatory conditions and/or diseases involving degradation of cartilage and/or disruption of cartilage homeostasis.
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Paragraph 0359
(2016/07/27)
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- Esters of 5-aminolevulinic acid as photosensitizing agents in photochemotherapy
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The present invention relates to compounds being esters of 5-aminolevulinic acids or pharmaceutically acceptable salts thereof, including compounds of formula (I) R22N—CH2COCH2-CH2CO—OR1 (wherein R1 may represent alkyl optionally substituted by hydroxy, alkoxy, acyloxy, alkoxycarbonyloxy, amino, aryl, oxo or fluoro groups and optionally interrupted by oxygen, nitrogen, sulphur or phosphorus atoms; and R2 represents a hydrogen atom or a group R1, and both R2 groups may be the identical or different), and their use in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body, and products and kits for performing the invention.
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- The synthesis and applications of 5-aminolevulinic acid (ALA) derivatives in photodynamic therapy and photodiagnosis
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A route has been developed to high-purity precursors, viz., ALA esters, to be used in photodiagnosis and photodynamic therapy. Hexyl, butyl and methyl 5-aminolevulinates are similar to the ALA acid in chemical stability and efficacy in producing the appropriate photosensitizer PpIX. Tests carried out on animal models showed the method based on the esters to be the more selective.
- Dabrowski, Zbigniew,Kwasny, Miroslaw,Kaminski, Jaroslaw,Beldowicz, Maria,Lewicka, Lidia,Obukowicz, Bozena,Kaliszewski, Miron,Pirozynska, Ewa
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p. 219 - 224
(2007/10/03)
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- The effects of 5-aminolevulinic acid esters on protoporphyrin IX production in human adenocarcinoma cell lines
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Photodynamic diagnosis (PDD) and photodynamic therapy (PDT) using 5-aminolevulinic acid (ALA)-induced protoporphyrin IX (PPIX) is an interesting approach to detect and treat dysplasia and early cancers in the gastrointestinal tract. Because of low lipophi
- Brunner,Hausmann,Krieg,Endlicher,Schoelmerich,Knuechel,Messmann
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p. 721 - 725
(2007/10/03)
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- Esters of 5-aminolevulinic acid as photosensitizing agents in photochemotherapy
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PCT No. PCT/GB96/00553 Sec. 371 Date Dec. 5, 1997 Sec. 102(e) Date Dec. 5, 1997 PCT Filed Mar. 8, 1996 PCT Pub. No. WO96/28412 PCT Pub. Date Sep. 19, 1996The invention provides a pharmaceutical compositions comprising a compound of formula I:R22N-CH2COCH2-CH2CO-OR1(I)wherein, R1 and R2 have any of the values defined in the specification; or a salt thereof; and a pharmaceutically acceptable carrier or excipient. The invention also provides a method for the diagnosis or photochemotherapeutic treatment of disorders or abnormalities of external or internal surfaces of the body using such compounds or salts.
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