1910803-72-3Relevant academic research and scientific papers
The Synthesis and Biological Evaluation of Some C-9 and C-10 Substituted Derivatives of the RNA Polymerase i Transcription Inhibitor CX-5461
Amarasiri, Madushani,Vo, Yen,Gardiner, Michael G.,Poh, Perlita,Soo, Priscilla,Pavy, Megan,Hein, Nadine,Ferreira, Rita,Hannan, Katherine M.,Hannan, Ross D.,Banwell, Martin G.
, p. 540 - 556 (2021/04/23)
The regio-isomeric alkynyl-substituted derivatives, 2 and 3, of the RNA Polymerase I (Pol I) transcription inhibitor CX-5461 (1) were prepared and the active one (compound 3) subjected to click reactions ([3 + 2]-cycloaddition reactions) with certain alkyl azides bearing biotin or fluorescent tags. Compounds 2 and 3, as well as four [3 + 2]-cycloadducts of the latter, were subjected to biological evaluation in a human acute myeloid leukemia cell line model. Among the six compounds tested only alkyne 3 remained active but this was less potent than parent 1.
Bilateral biotin-phthalocyanine zinc conjugate as well as preparation and application thereof
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Paragraph 0014, (2016/12/01)
The invention discloses a bilateral biotin-phthalocyanine zinc conjugate as well as preparation and application thereof. According to the conjugate disclosed by the invention, a biotin-cell growth-promoting factor (which is a critical micronutrient for cells to maintain normal functions, growth and reproduction) is used as a tumor target and is covalently connected onto a phthalocyanine zinc photosensitizer capable of being used for a photodynamic therapy, thus obtaining a third-generation anti-cancer photosensitizer for targeted therapy. Meanwhile, according to the conjugate, the biotin instead of a phthalocyanine zinc derivative acts a research object, human breast cancer cell MCF-7 and human embryo lung inoblast HELF act as subject cell lines respectively, a research regarding the in-vitro anti-cancer activity of the biotin is developed, and a prodrug suitable for a molecular targeted therapy is screened out, and a foundation is laid for applying the biotin instead of the phthalocyanine zinc derivative to the targeted therapy of cancers. The compound, namely the conjugate disclosed by the invention, is relatively simple in synthesis method, easily available in raw materials, low in cost, fewer in side reactions, relatively high in yield, easy to purify and beneficial for industrial production.
Rational design of biotin-disulfide-coumarin conjugates: A cancer targeted thiol probe and bioimaging
Jung, Danbi,Maiti, Sukhendu,Lee, Jae Hong,Lee, Joung Hae,Kim, Jong Seung
supporting information, p. 3044 - 3047 (2014/03/21)
Biotin-disulfide-coumarin conjugates are designed and synthesized as novel fluorescent sensors for cancer targeted intracellular thiol imaging in living organisms. In vitro experiments disclose that probe 6 is preferentially taken up by biotin receptor-positive A549 tumor cells through receptor mediated endocytosis. The Royal Society of Chemistry.
A fluorescence off-on reporter for real time monitoring of gemcitabine delivery to the cancer cells
Bhuniya, Sankarprasad,Lee, Min Hee,Jeon, Hyun Mi,Han, Ji Hye,Lee, Jae Hong,Park, Nayoung,Maiti, Sukhendu,Kang, Chulhun,Kim, Jong Seung
supporting information, p. 7141 - 7143 (2013/08/23)
We present the design, synthesis, optical properties and in vitro biological assessments of the theranostic prodrug 6 in which a near IR fluorophore is conjugated with a cancer cell-directing biotin unit; further it is linked with the anti-cancer drug gemcitabine via a self-immolative spacer, a disulfide bond. The prodrug 6 is able to monitor drug delivery and cellular imaging.
Design, synthesis, and biological evaluation of biotin-labeled (-)-ternatin, a potent fat-accumulation inhibitor against 3T3-L1 adipocytes
Shimokawa, Kenichiro,Yamada, Kaoru,Ohno, Osamu,Oba, Yuichi,Uemura, Daisuke
scheme or table, p. 92 - 95 (2009/04/16)
The design, synthesis, and biological activity of biotin-labeled (-)-ternatin are reported. Chemical modification, that is, biotinylation, was conducted using Click chemistry at the 6-position (NMe-d-ProGly moiety), which was a plausible location selected
