Conventional and microwave-assisted synthesis, anticancer evaluation, 99mTc-coupling and In-vivo study of some novel pyrazolone derivatives
Essa, Basma M; Selim, Adli A; Sayed, Galal H; Kurls Ekram Anwer;
Abstract
New pyrazolone derivatives were successfully synthesized by both microwave-assisted and conventional techniques. Compound 3 (3-(3-Methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)-3-oxopropanehydrazide) displayed remarkable anti-cancer activity (IC50 obtained at 8.71 and 10.63 µM for HCT-116 and MCF-7, respectively. Moreover, biodistribution study using radiolabeling approach revealed a remarked uptake of [99mTc]Tc-compound 3 complex into tumour induced in mice. The biodistribution showed high accumulation in tumour tissues with T/NT of 6.92 after 60 min post injection. As a result of these promising data, the newly synthesized compounds especially compound 3 affords a potential radio-carrier that could be used as a tumour marker and can be used for cancer therapy after further preclinical studies.
Other data
| Title | Conventional and microwave-assisted synthesis, anticancer evaluation, 99mTc-coupling and In-vivo study of some novel pyrazolone derivatives | Authors | Essa, Basma M; Selim, Adli A; Sayed, Galal H; Kurls Ekram Anwer | Keywords | (99m)Tc-coupling;HCT-116;MCF-7;Microwave;Pyrazolone;Syntheis | Issue Date | Aug-2022 | Publisher | ACADEMIC PRESS INC ELSEVIER SCIENCE | Journal | Bioorganic Chemistry | Volume | 125 | ISSN | 0045-2068 | DOI | 10.1016/j.bioorg.2022.105846 | PubMed ID | 35512493 | Scopus ID | 2-s2.0-85129259622 | Web of science ID | WOS:000800376400007 |
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