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Synthesis and biological evaluation of N, N-dialkylcarboxy coumarin-NO donor conjugates as potential anticancer agents.
Nelson, Grady L; Ronayne, Conor T; Solano, Lucas N; Jonnalagadda, Sravan K; Jonnalagadda, Shirisha; Schumacher, Tanner J; Gardner, Zachary S; Palle, Hithardha; Mani, Chinnadurai; Rumbley, Jon; Mereddy, Venkatram R.
Affiliation
  • Nelson GL; Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, USA.
  • Ronayne CT; Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, USA.
  • Solano LN; Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, USA.
  • Jonnalagadda SK; Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, USA.
  • Jonnalagadda S; Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, USA.
  • Schumacher TJ; Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, USA.
  • Gardner ZS; Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, USA.
  • Palle H; Department of Cell Biology and Biochemistry, Texas Tech University Health Sciences Center, Lubbock, TX 79430, USA.
  • Mani C; Department of Cell Biology and Biochemistry, Texas Tech University Health Sciences Center, Lubbock, TX 79430, USA.
  • Rumbley J; Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, USA; Department of Pharmacy Practice & Pharmaceutical Sciences, University of Minnesota, Duluth, MN 55812, USA.
  • Mereddy VR; Integrated Biosciences Graduate Program, University of Minnesota, Duluth, MN 55812, USA; Department of Pharmacy Practice & Pharmaceutical Sciences, University of Minnesota, Duluth, MN 55812, USA; Department of Chemistry and Biochemistry, University of Minnesota Duluth, Duluth, MN 55812, USA. Ele
Bioorg Med Chem Lett ; 52: 128411, 2021 11 15.
Article in En | MEDLINE | ID: mdl-34626786
A series of nitric oxide (NO) donor furoxan conjugates of N, N-dialkylcarboxy coumarins have been synthesized as potential anticancer agents. The synthesized compounds have been tested for their in vitro antiproliferative activities on various cancer and noncancerous cell lines. The candidate derivatives exhibit selectivity towards cancer cells with excellent activities in low nM to µM concentrations. In vitro mechanistic studies indicate that the candidate compounds generate substantial NO, inhibit colony formation, and cause apoptosis in cancer cells. A preliminary in vivo tolerance study of the lead candidate 10 in mice indicates that it is well-tolerated, evidenced by zero mortality and normal body weight gains in treated mice. Further translation of the lead derivative 10 using MDA-MB-231 based tumor xenograft model shows good tumor growth reduction.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Coumarins / Antineoplastic Agents / Nitric Oxide Limits: Animals / Female / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2021 Document type: Article Affiliation country: United States Country of publication: United kingdom

Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Coumarins / Antineoplastic Agents / Nitric Oxide Limits: Animals / Female / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2021 Document type: Article Affiliation country: United States Country of publication: United kingdom