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Patent / Dec 17, 2018
Boronated multifunctional targeting drug conjugates, their uses and methods for their preparation
Source:
WO 2018158582 20180907
Tri-​component multi-​functional boronated complexes (B-​complexes)​, featuring reversible covalent bonds, are described, which incorporate a drug;a water-​sol. moiety (e.g. polyethylene glycol (PEG) chains, cyclodextrins)​;and a targeting unit.ÌýA B-​complex core was assembled in one step, and proved to be stable in different biocompatible conditions, such as human plasma, though reversible for example in the presence of glutathione (GSH)​.ÌýThis platform enabled the modular construction of the multifunctional conjugates exhibiting high selectivity towards, for example, folate- receptor-​pos. MDA-​MB-​231 cancer cells, having an IC50 in the low nanomolar range.
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