134098-64-9Relevant academic research and scientific papers
Molecular umbrella as a nanocarrier for antifungals
Martynow, Dorota,Milewska, Maria J.,Milewski, S?awomir,Skwarecki, Andrzej S.
, (2021/09/20)
A molecular umbrella composed of two O‐sulfated cholic acid residues was applied for the construction of conjugates with cispentacin, containing a “trimethyl lock” (TML) or o‐dithiobenzylcarbamoyl moiety as a cleavable linker. Three out of five conjugates
A General Approach to Enzyme-Responsive Liposomes
Lou, Jinchao,Best, Michael D.
, p. 8597 - 8607 (2020/07/04)
Liposomes are effective nanocarriers due to their ability to deliver encapsulated drugs to diseased cells. Nevertheless, liposome delivery would be improved by enhancing the ability to control the release of contents at the target site. While various stimuli have been explored for triggering liposome release, enzymes provide excellent targets due to their common overexpression in diseased cells. We present a general approach to enzyme-responsive liposomes exploiting targets that are commonly aberrant in disease, including esterases, phosphatases, and β-galactosidases. Responsive lipids correlating with each enzyme family were designed and synthesized bearing an enzyme substrate moiety attached via a self-immolating linker to a non-bilayer lipid scaffold, such that enzymatic hydrolysis triggers lipid decomposition to disrupt membrane integrity and release contents. Liposome dye leakage assays demonstrated that each enzyme-responsive liposome yielded significant content release upon enzymatic treatment compared to minimal release in controls. Results also showed that fine-tuning liposome composition was critical for controlling release. DLS analysis showed particle size increases in the cases of esterase- and β-galactosidase-responsive lipids, supporting alterations to membrane properties. These results showcase an effective modular strategy that can be tailored to target different enzymes, providing a promising new avenue for advancing liposomal drug delivery.
NRTI THERAPIES
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, (2020/07/14)
Polymer-of-prodrug (POP) materials enable new nucleoside reverse transcriptase inhibitor (NRTI) therapy strategies. The materials are prodrugs of NRTIs in the form of polymers. Suitable materials include products which are polymeric NRTI delivery systems comprising polymeric materials which are capable of degradation after administration to release NRTIs or NRTI prodrugs which themselves are capable of metabolism to the parent NRTIs. The NRTIs may optionally be selected from tenofovir (TFV), emtricitabine (FTC), lamivudine (3TC) and MK-8591 (EFdA). The invention facilitates long-acting (LA) regimens. Constructs of the materials may be in the form of injectable compositions or implants.
COMPOUNDS USEFUL IN HIV THERAPY
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, (2020/09/20)
The invention relates to compounds of Formula (I), salts thereof, pharmaceutical compositions thereof, as well as methods of treating or preventing HIV in subjects.
MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE
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, (2019/07/19)
Provided are IDO1 inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases. Formula I Wherein R1 is a group having Formula II
INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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, (2019/07/20)
The present invention provides a compound of formula (II): an inhibitor of indoleamine 2,3-dioxygenase (IDO), which may be used as medicaments for the treatment of proliferative disorders, such as cancer, viral infections and/or autoimmune diseases. Its prodrugs are disclosed.
Combretastatin analogue water-soluble pre-- prodrug and its preparation method
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, (2017/08/25)
The invention relates to a combretastatin A-4 analogue pro-prodrug, and a preparation method thereof. The structure formula of the combretastatin A-4 analogue pro-prodrug is represented by a formula in the invention; and the combretastatin A-4 analogue pr
PRODRUGS OF 1,4-BENZODIAZEPINONE COMPOUNDS
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, (2014/04/04)
Disclosed are compounds of Formula (I) and salts thereof, wherein: a) R1 is H or CH3, and R2 is Ry; or b) R1 is Rx and R2 is H; wherein Rx and Ry are disclosed herein.
Novel trimethyl lock based enzyme switch for the self-assembly and disassembly of gold nanoparticles
Liu, Rongrong,Aw, Junxin,Teo, Weiling,Padmanabhan, Parasuraman,Xing, Bengang
, p. 594 - 598 (2010/06/18)
A novel trimethyl lock based dual enzyme-responsive gold nanoparticles (AuNPs) conjugate was developed to control the self-assembly and disassembly of AuNPs in one population of nanoparticles, which can be easily monitored by naked eye, simple spectrophot
ANTI-VIRAL COMPOUNDS
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, (2008/12/08)
Compounds effective in inhibiting replication of Hepatitis C virus ( HCV ) or other viruses are disclosed. This invention is also directed to compositions comprising such compounds, coformulation or co-administration of such compounds with other anti-viral or therapeutic agents, processes and intermediates for the syntheses of such compounds, and methods of using such compounds for the treatment of HCV or other viral infections.
