Abstract:
:The first example of vinca derivatives 16-18 able to modulate P-glycoprotein (Pgp) efflux activity is reported. They were elaborated in two steps from vinorelbine 3 (VLN) by a modification of the velbenamine moiety. These compounds were able to decrease efficiently Pgp mediated influx and efflux of rhodamine-123 (Rho) and to restore the cytotoxicity of vinorelbine 3 (VLN) and doxorubicin (Dox) on K562R (dox-resistant) cell lines.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Gherbovet O,García Alvarez MC,Bignon J,Roussi Fdoi
10.1021/acs.jmedchem.6b00525subject
Has Abstractpub_date
2016-12-08 00:00:00pages
10774-10780issue
23eissn
0022-2623issn
1520-4804journal_volume
59pub_type
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abstract::Novel tumor-targeting theranostic conjugates 1 and 2, bearing either a fluorine-labeled prosthetic as a potential (18)F-PET radiotracer (1) or a fluorescence probe (2) for internalization studies in vitro, were designed and synthesized. We confirmed efficient internalization of 2 in biotin-receptor positive (BR+) canc...
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journal_title:Journal of medicinal chemistry
pub_type: 杂志文章,评审
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abstract::In this paper, a peptide substrate (Pep8) of TSSK1 is identified. Using Pep8 as a substrate, two homogeneous and efficient assays for TSSK1 inhibitors screening have been developed, including luminescent kinase assay and LC-MS-based high-throughput assay. Two classes of compounds were identified that are able to effic...
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