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One-pot synthesis of cinnamylideneacetophenones and their in vitro cytotoxicity in breast cancer cells.
Weldon, David J; Saulsbury, Marilyn D; Goh, Joshua; Rowland, Leah; Campbell, Petreena; Robinson, Laijia; Miller, Calvin; Christian, Joshua; Amis, Louisa; Taylor, Nia; Dill, Cassandra; Davis, Willie; Evans, Stanley L; Brantley, Eileen.
Affiliation
  • Weldon DJ; Department of Pharmaceutical and Administrative Sciences, School of Pharmacy, Loma Linda University, Loma Linda, CA, United States.
  • Saulsbury MD; Department of Pharmaceutical Sciences, Hampton University, Hampton, VA, United States.
  • Goh J; Department of Pharmaceutical and Administrative Sciences, School of Pharmacy, Loma Linda University, Loma Linda, CA, United States.
  • Rowland L; Department of Basic Sciences, School of Medicine, Loma Linda University, Loma Linda, CA, United States.
  • Campbell P; Department of Basic Sciences, School of Medicine, Loma Linda University, Loma Linda, CA, United States.
  • Robinson L; Department of Basic Sciences, School of Medicine, Loma Linda University, Loma Linda, CA, United States; Department of Chemistry, Geology and Physics, School of Mathematics, Science & Technology, Elizabeth City State University, Elizabeth City, NC, United States.
  • Miller C; Department of Pharmaceutical and Administrative Sciences, School of Pharmacy, Loma Linda University, Loma Linda, CA, United States.
  • Christian J; Department of Pharmaceutical and Administrative Sciences, School of Pharmacy, Loma Linda University, Loma Linda, CA, United States.
  • Amis L; Department of Basic Sciences, School of Medicine, Loma Linda University, Loma Linda, CA, United States.
  • Taylor N; Department of Basic Sciences, School of Medicine, Loma Linda University, Loma Linda, CA, United States.
  • Dill C; Department of Basic Sciences, School of Medicine, Loma Linda University, Loma Linda, CA, United States.
  • Davis W; Department of Pharmaceutical and Administrative Sciences, School of Pharmacy, Loma Linda University, Loma Linda, CA, United States; Department of Basic Sciences, School of Medicine, Loma Linda University, Loma Linda, CA, United States.
  • Evans SL; Department of Neuroscience and Pharmacology, Meharry Medical College, Nashville, TN, United States.
  • Brantley E; Department of Pharmaceutical and Administrative Sciences, School of Pharmacy, Loma Linda University, Loma Linda, CA, United States; Department of Basic Sciences, School of Medicine, Loma Linda University, Loma Linda, CA, United States; Department of Chemistry, University of California, Riverside, CA
Bioorg Med Chem Lett ; 24(15): 3381-4, 2014 Aug 01.
Article in En | MEDLINE | ID: mdl-24957352
ABSTRACT
A series of cinnamylideneacetophenones were synthesized via a modified Claisen-Schmidt condensation reaction and evaluated for cytotoxicity against breast cancer cells using the Alamar Blue™ assay. Derivatives 17 and 18 bearing a 2-nitro group on the B ring, exhibited sub-micromolar cytotoxicity in MCF-7 cells (IC50=71 and 1.9 nM), respectively. Derivative 17 also displayed sub-micromolar (IC50=780 nM) cytotoxicity in MDA-MB-468 cells. Additionally, 17 and 18 displayed significantly less cytotoxicity than the chemotherapeutic doxorubicin in non-tumorigenic MCF-10A cells. This study provides evidence supporting the continued development of nitro-substituted cinnamylideneacetophenones as small molecules to treat breast cancer.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Ketones / Antineoplastic Agents / Nitrobenzenes Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2014 Document type: Article Affiliation country: United States
Fulltext
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Ketones / Antineoplastic Agents / Nitrobenzenes Limits: Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2014 Document type: Article Affiliation country: United States