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

被引：9

作者：

Shamsel-Din, Hesham A. ^{[1
,2
]}

Gizawy, Mohamed A. ^{[1
,2
]}

Abdelaziz, Gamal ^{[1
]}

机构：

[1] Atom Energy Author, Hot Labs Ctr, Labeled Cpds Dept, POB 13759, Cairo, Egypt

[2] Atom Energy Author, Egyptian Second Res Reactor ETRR 2, Radioisotopes Prod Facil RPF, POB 13759, Cairo, Egypt

来源：

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY | 2020年 / 326卷 / 02期

关键词：

Thidiazuron; Technetium-99m; Molecular docking; Cervical cancer; Sodium dithionite; IN-VITRO; TDZ;

D O I：

10.1007/s10967-020-07385-1

中图分类号：

O65 [分析化学];

学科分类号：

070302 ; 081704 ;

摘要：

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 [Tc-99m]technetium bisthiadiazuron (Tc-99m-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.

引用

页码：1375 / 1381

页数：7

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