Dodecaborate Conjugates Targeting Tumor Cell Overexpressing Translocator Protein for Boron Neutron Capture Therapy

Yoshihide Hattori; Miki Ishimura; Youichirou Ohta; Hiroshi Takenaka; Shinji Kawabata; Mitsunori Kirihata

doi:10.1021/acsmedchemlett.1c00377

Dodecaborate Conjugates Targeting Tumor Cell Overexpressing Translocator Protein for Boron Neutron Capture Therapy

ACS Med Chem Lett. 2021 Dec 1;13(1):50-54. doi: 10.1021/acsmedchemlett.1c00377. eCollection 2022 Jan 13.

Authors

Yoshihide Hattori¹, Miki Ishimura^{1

2}, Youichirou Ohta^{1

2}, Hiroshi Takenaka^{1

2}, Shinji Kawabata³, Mitsunori Kirihata¹

Affiliations

¹ Research Center of Boron Neutron Capture Therapy, Osaka Prefecture University, 1-1, Gakuen-cho, Naka-ku, Sakai, Osaka 599-8531, Japan.
² Stella Pharma Co., ORIX Kouraibashi Bldg., 3-2-7 Kouraibashi, Chuo-ku, Osaka 541-0043, Japan.
³ Department of Neurosurgery, Osaka Medical and Pharmaceutical University, 2-7 Daigaku-machi, Takatsuki-shi, Osaka 569-8686, Japan.

Abstract

We developed novel closo-dodecaborate ([B₁₂H₁₁]^2-) anion-containing translocator protein (TSPO) ligand as a boron carrier for boron neutron capture therapy. This compound shows high water solubility and can deliver boron to TSPO highly expressed in breast cancer cells. We describe the synthesis and in vitro evaluation of a dodecaborate-based pyrazolopyrimidine.