Synthesis and antitumor activity of novel RRx-001 derivatives

VernacularTitle:RRx-001衍生物的合成和抗肿瘤活性研究
Author: Ruonan WU ¹ ; Wenmin TANG ^{2
,

3} ; Lin GAO ¹ ; Yuelin WU ³ ; Chuan LUO ¹ ; Zhenyuan MIAO ⁴
Author Information

1. Anhui Huarun Golden Frog Pharmaceutical Ltd., Huaibei 235000, China.
2. School of Pharmacy, Naval Medical University, Shanghai 200433, China
3. School of Chemical and Environmental Engineering, Shanghai Institute of Technology, Shanghai 201418, China.
4. School of Pharmacy, Naval Medical University, Shanghai 200433, China.
Publication Type:Originalarticles
Keywords: RRx-001; immuno-oncology; covalent inhibitor; synthesis; antitumor
From: Journal of Pharmaceutical Practice and Service 2025;43(8):400-403
CountryChina
Language:Chinese
Abstract: Objective To study the antitumor activities of RRx-001 derivatives with novel covalent fragments. Methods Four targeted compounds were designed and synthesized. The structures were confirmed by ¹H NMR and HRMS. A549 and HCT116 cancer cell lines were selected for antiproliferative activity assays. Results All the compounds revealed antitumor activities and compound ZM528 showed the best antitumor activity against these two cell lines with IC₅₀ values of （5.1±4.8） μmol/L and （6.0±2.7） μmol/L, respectively. Conclusion The result indicated that bromoacetyl group of RRx-001 could be substituted with other covalent fragments.