Published November 2020 | Version v1
Journal article

Molecular docking and preliminary bioevaluation of 99mTc-Thiadiazuron as a novel potential agent for cervical cancer imaging

  • 1. Atomic Energy Authority, Cairo (Egypt). Radioisotopes Production Facility (RPF), Egyptian Second Research Reactor (ETRR-2)
  • 2. Atomic Energy Authority, Cairo (Egypt). Labeled Compounds Department, Hot Labs Center

Description

Thidiazuron (TDZ) was reported to possess anti-cancer activity against Human cervical carcinoma cell line, so that this study has been conducted for the radiolabeling of TDZ with Technetium-99m. The conditions of the radiolabeling process were optimized and a high radiochemical yield of 93.1 ± 0.35% has been obtained. Molecular docking study illustrated that [99mTc]technetium bisthiadiazuron (99mTc-TDZ) complex has the ability to bind with Caspase-3 protein that over expressed in cancers. Its in-vivo biodistribution on solid tumor bearing mice showed comparatively high T/NT ratio of 6.87 ± 0.14 at 60 min post injection. These promising characteristics make our new designed labeled conjugate a very suitable candidate for molecular imaging of solid tumors, particularly in the cervix. (author)

Additional details

Publishing Information

Journal Title
Journal of Radioanalytical and Nuclear Chemistry
Journal Volume
326
Journal Issue
2
Journal Page Range
p. 1375-1381
ISSN
0236-5731
CODEN
JRNCDM

Optional Information

Notes
26 refs.