Activity of 2-aryl-2-(3-indolyl)acetohydroxamates against drug-resistant cancer cells

Alexander V. Aksenov, Alexander N. Smirnov, Igor V. Magedov, Mary R. Reisenauer, Nicolai A. Aksenov, Inna V. Aksenova, Alexander L. Pendleton, Gina Nguyen, Robert K. Johnston, Michael Rubin, Annelise De Carvalho, Robert Kiss, Véronique Mathieu, Florence Lefranc, Jaime Correa, David A. Cavazos, Andrew J. Brenner, Brad A. Bryan, Snezna Rogelj, Alexander KornienkoLiliya V. Frolova

Research output: Contribution to journalArticlepeer-review

51 Scopus citations


Many types of tumor, including glioma, melanoma, non-small cell lung, esophageal, and head and neck cancer, among others, are intrinsically resistant to apoptosis induction and poorly responsive to current therapies with proapoptotic agents. In addition, tumors often develop multidrug resistance based on the cellular efflux of chemotherapeutic agents. Thus, novel anticancer agents capable of overcoming these intrinsic or developed tumor resistance mechanisms are urgently needed. We describe a series of 2-aryl-2-(3-indolyl)acetohydroxamic acids that are active against apoptosis-and multidrug-resistant cancer cells as well as glioblastoma neurosphere stemlike cell cultures derived from patients. Thus, the described compounds serve as a novel chemical scaffold for the development of potentially highly effective clinical cancer drugs.

Original languageEnglish (US)
Pages (from-to)2206-2220
Number of pages15
JournalJournal of Medicinal Chemistry
Issue number5
StatePublished - Mar 12 2015

ASJC Scopus subject areas

  • Drug Discovery
  • Molecular Medicine


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