1. Synthesis of Selenium-Quinone Hybrid Compounds with Potential Antitumor Activity via Rh-Catalyzed C-H Bond Activation and Click Reactions.
- Author
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Jardim GAM, Lima DJB, Valença WO, Lima DJB, Cavalcanti BC, Pessoa C, Rafique J, Braga AL, Jacob C, da Silva Júnior EN, and da Cruz EHG
- Subjects
- Antineoplastic Agents therapeutic use, Catalysis, Cell Line, Tumor, Cell Proliferation drug effects, Cell Survival drug effects, Click Chemistry, Drug Screening Assays, Antitumor, Humans, Organoselenium Compounds pharmacology, Structure-Activity Relationship, Triazoles pharmacology, Antineoplastic Agents chemical synthesis, Organoselenium Compounds chemical synthesis, Quinones chemistry, Rhodium chemistry, Triazoles chemical synthesis
- Abstract
In continuation of our quest for new redox-modulating catalytic antitumor molecules, selenium-containing quinone-based 1,2,3-triazoles were synthesized using rhodium-catalyzed C-H bond activation and click reactions. All compounds were evaluated against five types of cancer cell lines: HL-60 (human promyelocytic leukemia cells), HCT-116 (human colon carcinoma cells), SF295 (human glioblastoma cells), NCIH-460 (human lung cells) and PC3 (human prostate cancer cells). Some compounds showed good activity with IC
50 values below 1 µM. The cytotoxic potential of the naphthoquinoidal derivatives was also evaluated in non-tumor cells, exemplified by L929 cells. Overall, these compounds represent promising new lead derivatives and stand for a new class of chalcogenium-containing derivatives with potential antitumor activity., Competing Interests: The authors declare no conflict of interest.- Published
- 2017
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