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Synthesis and evaluation of an imidazole derivative–fluorescein conjugate
Bioorganic & Medicinal Chemistry, 2013The murine double minute (MDM2) oncogene a negative regulator of protein 53 (p53) tumor suppressor, is found overexpressed in many different types of cancer and the interaction between MDM2 and p53 has become the target of intensive research. MDM2 inhibitors represent a promising class of p53 activating compounds that may be effective in cancer ...
Pradip, Ghosh +3 more
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Synthesis and biological evaluation of PEG-tirofiban conjugates
Bioorganic & Medicinal Chemistry Letters, 2008We have conjugated tirofiban, an antagonist of the GPIIb/IIIa integrin receptor, to PEG, and shown that these polymers effectively inhibit platelet aggregation. This inhibition decreased with the size of the polymer. Our goal was to develop new cryoprotective agents to store frozen platelets.
Laurent, Désaubry +3 more
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Synthesis and evaluation of a DHA and 10-hydroxycamptothecin conjugate
Bioorganic & Medicinal Chemistry, 2005We have synthesized a conjugate of cis-4,7,10,13,16,19-docosahexenoic acid (DHA) and 10-hydroxycamptothecin (HCPT), DHA-HCPT. The antitumor activity of DHA-HCPT was evaluated in vitro against L1210 leukemia cells and in experimental animal tumor models including L1210 leukemia, Lewis lung carcinoma, and colon 38 adenocarcinoma.
Yuqiang, Wang +3 more
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Quantitative evaluation of phase-conjugate novelty filters
Optics Letters, 1991A Michelson interferometer whose signal arm is terminated by a self-pumped BaTiO(3) phase conjugator records phase-change distributions in times short compared with the conjugator rewrite time that correspond quantitatively to a single (not a double) traversal of the phase disturbance.
F C, Jahoda, P R, Forman, B L, Mason
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Immunological evaluation of SW–HSA conjugate on goats
Colloids and Surfaces B: Biointerfaces, 2007Locoweeds cause significant livestock poisoning and economic loss all over the world. The purpose of this study was to investigate the immune effects of locoweed toxin, swainsonine (SW) and human serum albumin (HSA) conjugate (SW-HSA), on goats. Twenty-four Sannon goats were randomly separated into immune control group (eight goats), immune poisoning ...
Dewen, Tong +9 more
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Economic evaluation of pneumococcal conjugate vaccination in Finland
Scandinavian Journal of Infectious Diseases, 2005The aim of this study was to evaluate cost-effectiveness of pneumococcal conjugate vaccine (PCV7) in children
Heini, Salo +6 more
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Synthesis and biological evaluation of nandrolone–bodipy conjugates
Steroids, 2015Here, we report synthesis and biological evaluation of fluorescent nandrolone-3-carboxymethyloxime derivatives conjugated with green-emitting bodipy dye via PEG linkers. All the newly-synthesized compounds were evaluated for their effect on cell proliferation in vitro in MCF-7, LNCaP, PC-3 and HEK 293T model cell lines using WST-1 assay.
Michal, Jurášek +5 more
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Bioconjugate Chemistry, 1990
The preparations and conjugations of 2,3,5,6-tetrafluorophenyl 5-[125I/131I]iodo-4-pentenoate (7a) and 2,3,5,6-tetrafluorophenyl 3,3-dimethyl-5-[125I/131I]iodo-4-pentenoate (7b) to monoclonal antibodies are reported. Reagents 7a and 7b were prepared in high radiochemical yield by iododestannylation of their corresponding 5-tri-n-butylstannyl precursors.
S W, Hadley, D S, Wilbur
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The preparations and conjugations of 2,3,5,6-tetrafluorophenyl 5-[125I/131I]iodo-4-pentenoate (7a) and 2,3,5,6-tetrafluorophenyl 3,3-dimethyl-5-[125I/131I]iodo-4-pentenoate (7b) to monoclonal antibodies are reported. Reagents 7a and 7b were prepared in high radiochemical yield by iododestannylation of their corresponding 5-tri-n-butylstannyl precursors.
S W, Hadley, D S, Wilbur
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Synthesis and evaluation of fluorescent Pam3Cys peptide conjugates
Bioorganic & Medicinal Chemistry Letters, 2016Chirally pure R- and S-epimers of TLR2 ligand Pam3CysSK4 were prepared and separately conjugated to an OVA model epitope, in which lysine was replaced by azidonorleucine. The azide function in the conjugate permitted labelling with different fluorophores by use of strain-promoted 3+2 cycloaddition.
Gential, G.P. +7 more
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Angewandte Chemie, 2022
AbstractDrug repurposing is considered a promising strategy to fight antimicrobial resistance (AMR). Methotrexate (Mtx), a classical anticancer drug, could strongly inhibit bacterial dihydrofolate reductase (DHFR). However, its poor permeability into bacteria and potent human cytotoxicity make it unsuitable as an antibacterial.
Sheng Zhao +11 more
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AbstractDrug repurposing is considered a promising strategy to fight antimicrobial resistance (AMR). Methotrexate (Mtx), a classical anticancer drug, could strongly inhibit bacterial dihydrofolate reductase (DHFR). However, its poor permeability into bacteria and potent human cytotoxicity make it unsuitable as an antibacterial.
Sheng Zhao +11 more
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