Binary Drug Reinforced First Small-Molecule-Based Prodrug for Synergistic Anticancer Effects

Paramesh Jangili; Miae Won; Seo Jin Kim; Jieun Chun; Inseob Shim; Chulhun Kang; Wen Xiu Ren; Jong Seung Kim

doi:10.1021/acsabm.9b00418

Binary Drug Reinforced First Small-Molecule-Based Prodrug for Synergistic Anticancer Effects

ACS Appl Bio Mater. 2019 Aug 19;2(8):3532-3539. doi: 10.1021/acsabm.9b00418. Epub 2019 Jul 5.

Authors

Paramesh Jangili¹, Miae Won¹, Seo Jin Kim², Jieun Chun², Inseob Shim¹, Chulhun Kang², Wen Xiu Ren^{3

4}, Jong Seung Kim¹

Affiliations

¹ Department of Chemistry, Korea University, Seoul 02841, Republic of Korea.
² Graduate School of East-West Medical Science, Kyung Hee University, Yongin 446-701, Republic of Korea.
³ Department of Radiology, The Affiliated Hospital of Southwest Medical University, Luzhou, Sichuan 646000, People's Republic of China.
⁴ Nuclear Medicine and Molecular Imaging Key Laboratory of Sichuan Province, Luzhou, Sichuan 646000, People's Republic of China.

PMID: 35030740
DOI: 10.1021/acsabm.9b00418

Abstract

We developed a small-molecule-based binary drug delivery system (BDDS) with two anticancer drugs, SN-38 and 5'-DFUR. The drug release from the prodrug BDDS can be achieved upon its reaction with intracellular H₂O₂, overexpressed in cancer cells. The efficacy of BDDS was demonstrated by a comparative study along with that of a single drug conjugate (SDDS), bearing SN-38 alone.

Keywords: 5′-DFUR; COX-2; SN-38; binary drug; synergistic effect.