Synthesis and biological evaluation of new water-soluble photoactive chlorin conjugate for targeted delivery.
Тип публикации: Journal Article
Дата публикации: 2018-01-01
scimago Q1
wos Q1
БС1
SJR: 1.151
CiteScore: 11.7
Impact factor: 5.9
ISSN: 02235234, 17683254
PubMed ID:
29291441
Organic Chemistry
Drug Discovery
General Medicine
Pharmacology
Краткое описание
A new water-soluble conjugate, consisting of a chlorin-based photosensitizing part, and a 4-arylaminoquinazoline moiety with high potential affinity to an epidermal growth factor receptors (EGFR) and vascular endothelial growth factor receptors (VEGFR), suitable for photodynamic therapy (PDT), was synthesized starting from methylpheophorbide-a in seven steps. An increased accumulation of this compound in A431 cells with high level of EGFR expression, in comparison with CHO and HeLa cells with low EGFR expression was observed. The prepared conjugate exhibits dark and photoinduced cytotoxicity at micromolar concentrations with IC50dark/IC50light ratio of 11-18. In tumor-bearing mice, the conjugate preferentially accumulates in the tumor tissue.
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ГОСТ
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Otvagin V. F. et al. Synthesis and biological evaluation of new water-soluble photoactive chlorin conjugate for targeted delivery. // European Journal of Medicinal Chemistry. 2018. Vol. 144. pp. 740-750.
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Otvagin V. F., Nyuchev A. V., Kuzmina N. S., Grishin I. D., Gavryushin A. E., Romanenko Y. V., Koifman O. I., Belykh D. V., Peskova N. N., Shilyagina N. Yu., Balalaeva I. V., Schmalz H. Synthesis and biological evaluation of new water-soluble photoactive chlorin conjugate for targeted delivery. // European Journal of Medicinal Chemistry. 2018. Vol. 144. pp. 740-750.
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RIS
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TY - JOUR
DO - 10.1016/j.ejmech.2017.12.062
UR - https://doi.org/10.1016/j.ejmech.2017.12.062
TI - Synthesis and biological evaluation of new water-soluble photoactive chlorin conjugate for targeted delivery.
T2 - European Journal of Medicinal Chemistry
AU - Otvagin, Vasilii F
AU - Nyuchev, Alexander V.
AU - Kuzmina, Natalia S
AU - Grishin, Ivan D.
AU - Gavryushin, Andrei E
AU - Romanenko, Yuliya V
AU - Koifman, Oskar I.
AU - Belykh, Dmitrii V.
AU - Peskova, Nina N
AU - Shilyagina, Natalia Yu
AU - Balalaeva, Irina V.
AU - Schmalz, H.-G.
PY - 2018
DA - 2018/01/01
PB - Elsevier
SP - 740-750
VL - 144
PMID - 29291441
SN - 0223-5234
SN - 1768-3254
ER -
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BibTex (до 50 авторов)
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@article{2018_Otvagin,
author = {Vasilii F Otvagin and Alexander V. Nyuchev and Natalia S Kuzmina and Ivan D. Grishin and Andrei E Gavryushin and Yuliya V Romanenko and Oskar I. Koifman and Dmitrii V. Belykh and Nina N Peskova and Natalia Yu Shilyagina and Irina V. Balalaeva and H.-G. Schmalz},
title = {Synthesis and biological evaluation of new water-soluble photoactive chlorin conjugate for targeted delivery.},
journal = {European Journal of Medicinal Chemistry},
year = {2018},
volume = {144},
publisher = {Elsevier},
month = {jan},
url = {https://doi.org/10.1016/j.ejmech.2017.12.062},
pages = {740--750},
doi = {10.1016/j.ejmech.2017.12.062}
}
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