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Radiochemistry of Therapeutic Radionuclides
Published in David M. Goldenberg, Cancer Therapy with Radiolabeled Antibodies, 1995
A procedure involving a different type of iodinated intermediate, tyramine cellobiose, has also been described.48 This agent has been used to label MoAbs by cyanuric chloride activation, and the conjugate was shown to be resistant to intracellular deiodination in vivo. The sugar group is nonmetabolizable, and it was claimed that with iodinated MoAbs prepared with this methodology iodine was retained in tumor for a longer period than iodine attached to MoAbs using the Chloramine-T procedure.48
Discovery of novel enasidenib analogues targeting inhibition of mutant isocitrate dehydrogenase 2 as antileukaemic agents
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Ahmed F. Khalil, Tarek F. El-Moselhy, Eman A. El-Bastawissy, Rasha Abdelhady, Nancy S. Younis, Mervat H. El-Hamamsy
Target compounds, of series (I), 6a–l, and series (II), 7a–l were prepared as displayed in Scheme 1. The three chlorine atoms of cyanuric chloride, 1 disclosed diverse reactivity and can be substituted gradually at different temperatures38. Compounds 3a,b were prepared from cyanuric chloride 1via nucleophilic substitution of the first chlorine atom with morpholine, 2a or piperidine, 2b at 0–5 °C to afford analogues, 3a and 3b, respectively. Compounds 3a,b underwent nucleophilic substitution of the remaining two chlorine atoms with two hydrazine groups through heating under reflux with excess amount of hydrazine hydrate to provide the trisubstituted s-triazine derivatives, 4a,b, respectively. Condensation of hydrazine derivatives, 4a,b with various aldehydes yielded the corresponding hydrazones, 6a–l and 7a–l, respectively.
Ultrasound-sensitive cRGD-modified liposomes as a novel drug delivery system
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2022
Nour M. AlSawaftah, Vinod Paul, Doua Kosaji, Leen Khabbaz, Nahid S. Awad, Ghaleb A. Husseini
The thin-film hydration method was used to prepare the liposomes [24]. DPPC, DSPE-PEG(2000)-NH2, and cholesterol were added to a round-bottom flask at molar ratios of 65:5:30, respectively. Chloroform (4 ml) was then added to dissolve the lipids and evaporated while rotating under a vacuum at 50 °C for 20 min. A lipid film was formed, and 2 ml of the calcein, dissolved in PBS buffer (30 mM), was added to hydrate the lipid film using the rotatory evaporator. Unilamellar liposomes were formed using a sonicating bath (35 kHz) for 2 min (Elma D-78224, Melrose Park, Illinois, USA). The liposomes were then extruded using an extruder containing 200-nm polycarbonate filters (Avanti Polar Lipids, Inc., Alabaster, AL, USA). Unencapsulated calcein was removed by passing the liposomes through a gel filtration medium (Sephadex G-100). cRGD was conjugated to the liposomes using cyanuric chloride (2,4,6 trichloro-1,3,5 triazine) as a coupling agent, 10 mg of cyanuric chloride were dissolved in 500 µl of acetone and 1 ml of deionized water. It was added to the liposomes in a 1:1 molar ratio (cRGD: DSPE-PEG(2000)-NH2). The reaction was left to stir for 3 h at 2 °C. Three hundred and forty-six microlitres of the cRGD solution (5 mg of cRGD dissolved in 1 ml of borate buffer at pH∼8.5) were added to the mixture and were left stirring overnight. The preferential order for incorporating nucleophiles in cyanuric chloride was found to be alcohol > thiol > amine [25]. The expected coupling reaction is shown in Figure 2. The same volume of cyanuric chloride was added to the control and conjugated liposomes. The only difference is that the cRGD solution (prepared in borate buffer) was not added to the control liposomes. Instead, the same volume of pure borate buffer was added to the control liposomes. Both types of liposomes were then incubated under the same reaction conditions. Finally, gel filtration removed unconjugated cRGD, and the collected fractions were stored at 4 °C until further use.