Details

Autor(en) / Beteiligte

• Dhyani, Manish V
• Satpati, Drishty
• Korde, Aruna
• Sarma, Haladhar Dev
• Kumar, Chandan
• Banerjee, Sharmila

Titel

Preparation and preliminary bioevaluation of99m Tc(CO)3 -11β-progesterone derivative prepared via click chemistry route

Ist Teil von

• Nuclear medicine and biology, 2010, Vol.37 (8), p.997-1004

Erscheinungsjahr

2010

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• Abstract Introduction Progesterone receptors (PRs) overexpressed in breast cancers serve as potential targets for developing radiotracers for use in nuclear medicine. Hence, suitably derivatized progesterone can be envisaged as a potential vector for targeting overexpression of receptors in breast cancer. In the present article, we report the preparation of a99m Tc(CO)3 -progesterone triazole using the Cu(I)-catalyzed novel click chemistry route. Preliminary evaluation of the radiolabeled derivative has been carried out in binding studies with MCF 7 cell lines. Methods 11-Hydroxyprogesterone has been synthetically derivatized to 11-azidoprogesterone. Subsequently, the cycloaddition reaction between progesterone azide and propargyl glycine was carried out to prepare 1,4-bifunctionalized progesterone triazole analogue. The clicked progesterone triazole derivative was radiolabeled with99m Tc and characterized by HPLC. The chemical characterization of99m Tc(CO)3 -progesterone triazole has been carried out by preparing its corresponding rhenium complex using the [NEt4 ]2 [Re(CO)3 Br3 ] precursor. While in vitro studies were carried out in MCF7 cell lines, in vivo distribution studies were performed in female Swiss mice. Results The radiolabeled complex could be prepared in >95% radiochemical yield as determined by HPLC. In vitro studies of99m Tc(CO)3 -progesterone complex in MCF7 cell lines overexpressing receptors for breast cancer showed binding up to 30%. In vivo distribution studies in female Swiss mice have shown uterine uptake of 0.41 (0.06) % ID/g at 3 h postinjection (pi) and retention therein till 24 h pi. Conclusion The present study demonstrates a novel and facile route for preparation of99m Tc-labeled progesterone complex using click chemistry. This strategy can be further extended towards preparation of radiolabeled complexes of other steroidal derivatives.