Synthesis, 99m Tc-radiolabeling and in vivo evaluation of a new sulphonamide derivative for solid tumor imaging
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Synthesis, 99mTc‑radiolabeling and in vivo evaluation of a new sulphonamide derivative for solid tumor imaging H. A. Shamsel‑Din1 · E. G. Zaki2 Received: 14 February 2020 © Akadémiai Kiadó, Budapest, Hungary 2020
Abstract A novel sulphonamide derivative (EPBS) was prepared at high yield and characterized by 1H NMR and infrared radiation spectroscopy. Its cytotoxic activity was examined in breast carcinoma (MCF-7) cells at a dose of 25 μg/mL. Approximately 68 percent effective inhibition has been achieved. Furthermore, the synthesized ligand was directly radiolabeled with technetium-99m using sodium borohydride. High radiochemical purities (95.5%) were determined using radio-paper chromatography and electrophoresis. Its in vivo evaluation in tumor bearing mice demonstrated a high tumor uptake of the 99m Tc-EPBS complex at 30 min post injection (6.74%) and tumor/muscle (T/NT) ratio equal to 5.04 ± 0.05. In conclusion, 99m Tc-EPBS agent showed favorable characteristics for the radio-diagnosis of solid tumors. Keywords Sulphonamide · Technetium-99m · Sodium borohydride · Cancer · Radiodiagnosis
Introduction Significant improvement of treatment plans for cancer patients depends on the speed and accuracy of the diagnosis. New and effective agents for the diagnosis and treatment of tumors must be developed to achieve this objective [1, 2]. Sulfonamide agents are effective against bacterial infections and, in addition to anti-carbon anhydrase and metallic matrix protein (MMP), suppression of Nf-Y transcription activator, angiogenesis, and cause cell cycle disruption in the G1 phase. Antitumor, anti-inflammatory and antiviral activity has recently been reported for various synthesized sulphonamides [3–7]. On the other hand, the development of high selective radiopharmaceuticals in tumor tissues with a higher target/nontarget ratio (T/NT) than 1.5 is a challenge for specified tumor diagnostic agents with good potential [8–12]. 99mTc-radiopharmaceuticals have been an important diagnostic factor in nuclear medicine, depending on the most appropriate radionuclide (99mTc) with shorter half-life (6.02 h) and excellent * H. A. Shamsel‑Din [email protected] 1
Labeled Compounds Department, Hot Labs Center, Atomic Energy Authority, P.O. Box 13759, Cairo, Egypt
Egyptian Petroleum Research Institute, P.O. Box 11727, Nasr City, Cairo, Egypt
2
energy (142 keV) for SPECT (Single Photon Emission Computed Tomography). Generally, 99mTc-radiolabelling process performed by direct reduction technique of stannous salts to convert sodium pertechnetate ( Na99mTcO4) to 99mTc lower valence but undesired radiocolloids are generated during reaction. However, sodium borohydride has been shown to be an effective reducing tool in the preparation of radiopharmaceuticals without radiocolloids. Several 99mTc radiotracers have recently been prepared and regulatory approvals for tumor diagnostic techniques have been obtained. However, several 99mTc developed radiotracers [13–21] have been reported in literature and have some disadvantages, s
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