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Design, Synthesis, and Cancer Cell Growth Inhibitory Activity of Triphenylphosphonium Derivatives of the Triterpenoid Betulin

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dc.contributor.author Tsepaeva O.
dc.contributor.author Nemtarev A.
dc.contributor.author Abdullin T.
dc.contributor.author Grigor'Eva L.
dc.contributor.author Kuznetsova E.
dc.contributor.author Akhmadishina R.
dc.contributor.author Ziganshina L.
dc.contributor.author Cong H.
dc.contributor.author Mironov V.
dc.date.accessioned 2018-04-05T07:09:14Z
dc.date.available 2018-04-05T07:09:14Z
dc.date.issued 2017
dc.identifier.issn 0163-3864
dc.identifier.uri http://dspace.kpfu.ru/xmlui/handle/net/129597
dc.description.abstract © 2017 The American Chemical Society and American Society of Pharmacognosy. A series of new triphenylphosphonium (TPP) derivatives of the triterpenoid betulin (1, 3-lup-20(29)-ene-3β,28-diol) have been synthesized and evaluated for cytotoxic effects against human breast cancer (MCF-7), prostate adenocarcinoma (PC-3), vinblastine-resistant human breast cancer (MCF-7/Vinb), and human skin fibroblast (HSF) cells. The TPP moiety was applied as a carrier group through the acyl linker at the 28- or 3- and 28-positions of betulin to promote cellular and mitochondrial accumulation of the resultant compounds. A structure-activity relationship study has revealed the essential role of the TPP group in the biological properties of the betulin derivatives produced. The present results showed that a conjugate of betulin with TPP (3) enhanced antiproliferative activity toward vinblastine-resistant MCF-7 cells, with an IC 50 value as low as 0.045 μM.
dc.relation.ispartofseries Journal of Natural Products
dc.title Design, Synthesis, and Cancer Cell Growth Inhibitory Activity of Triphenylphosphonium Derivatives of the Triterpenoid Betulin
dc.type Article
dc.relation.ispartofseries-issue 8
dc.relation.ispartofseries-volume 80
dc.collection Публикации сотрудников КФУ
dc.relation.startpage 2232
dc.source.id SCOPUS01633864-2017-80-8-SID85028342968


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  • Публикации сотрудников КФУ Scopus [24551]
    Коллекция содержит публикации сотрудников Казанского федерального (до 2010 года Казанского государственного) университета, проиндексированные в БД Scopus, начиная с 1970г.

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