2. Academic Validation
  3. Novel Microtubule-Targeting 7-Deazahypoxanthines Derived from Marine Alkaloid Rigidins with Potent in Vitro and in Vivo Anticancer Activities

Novel Microtubule-Targeting 7-Deazahypoxanthines Derived from Marine Alkaloid Rigidins with Potent in Vitro and in Vivo Anticancer Activities

  • J Med Chem. 2016 Jan 14;59(1):480-5. doi: 10.1021/acs.jmedchem.5b01426.
Derek C Medellin 1,  Qiong Zhou 2,  Robert Scott 1,  R Matthew Hill 1,  Sarah K Frail 3,  Ramesh Dasari 1,  Steven J Ontiveros 4,  Stephen C Pelly 5,  Willem A L van Otterlo 5,  Tania Betancourt 1 6,  Charles B Shuster 4,  Ernest Hamel 7,  Ruoli Bai 7,  Daniel V LaBarbera 2,  Snezna Rogelj 3,  Liliya V Frolova 3,  Alexander Kornienko 1
Affiliations

Affiliations

  • 1 Department of Chemistry and Biochemistry, Texas State University , San Marcos, Texas 78666, United States.
  • 2 Department of Pharmaceutical Sciences, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of Colorado Anschutz Medical Campus , Aurora, Colorado 80045, United States.
  • 3 Departments of Chemistry and Biology, New Mexico Tech , Socorro, New Mexico 87801, United States.
  • 4 Department of Biology, New Mexico State University , Las Cruces, New Mexico 88003, United States.
  • 5 Department of Chemistry and Polymer Science, Stellenbosch University , Stellenbosch, Western Cape, South Africa.
  • 6 Materials Science, Engineering, and Commercialization Program, Texas State University , San Marcos, Texas 78666, United States.
  • 7 Screening Technologies Branch, Developmental Therapeutics Program, National Cancer Institute, Frederick National Laboratory of Cancer Research, National Institutes of Health, Frederick, Maryland 21702, United States.
PMID: 26641132 DOI: 10.1021/acs.jmedchem.5b01426
Abstract

Docking studies of tubulin-targeting C2-substituted 7-deazahypoxanthine analogues of marine alkaloid rigidins led to the design and synthesis of compounds containing linear C2-substituents. The C2-alkynyl analogue was found to have double- to single-digit nanomolar antiproliferative IC50 values and showed statistically significant tumor size reduction in a colon Cancer mouse model at nontoxic concentrations. These results provide impetus and further guidance for the development of these rigidin analogues as Anticancer agents.

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