4.4 Article

Synthesis of Quinone-Based N-Sulfonyl-1,2,3-triazoles: Chemical Reactivity of Rh(II) Azavinyl Carbenes and Antitumor Activity

Journal

CHEMISTRYSELECT
Volume 2, Issue 16, Pages 4301-4308

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/slct.201700885

Keywords

Cancer; Click Chemistry; Quinones; Rhodium(II) Azavinyl carbenes; Triazoles

Funding

  1. CNPq [474797/2013-9, PVE 401193/2014-4, PQ 305385/2014-3]
  2. Chamada Universal MCTI/CNPq [01/2016]
  3. FAPEMIG [01/2014 APQ-02478-14]
  4. CAPES
  5. INCT-Catalise
  6. CAPES [99999.008126/2015-01]
  7. DAAD [99999.008126/2015-01]

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Quinone-based N-sulfonyl-1,2,3-triazoles were synthesized by click chemistry and subsequently evaluated against eight types of cancer cell lines. Some of the compounds exhibited potent cytotoxicity with IC50 values < 1.0 mu M. Also, the cytotoxic potential of the quinones was evaluated against peripheral blood mononuclear (PBMC) and V79 cells. Additionally, the chemical reactivity of Rh(II) aza-vinyl carbenes generated in situ from these triazoles was studied. These compounds could provide promising new lead derivatives for more potent anticancer drug development.

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