2. Academic Validation
  3. Macrocyclic hexaoxazoles: Influence of aminoalkyl substituents on RNA and DNA G-quadruplex stabilization and cytotoxicity

Macrocyclic hexaoxazoles: Influence of aminoalkyl substituents on RNA and DNA G-quadruplex stabilization and cytotoxicity

  • Bioorg Med Chem Lett. 2010 May 15;20(10):3150-4. doi: 10.1016/j.bmcl.2010.03.086.
Mavurapu Satyanarayana 1,  Young-Ah Kim,  Suzanne G Rzuczek,  Daniel S Pilch,  Angela A Liu,  Leroy F Liu,  Joseph E Rice,  Edmond J LaVoie
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Rutgers, The State University of New Jersey, Piscataway, NJ 08854-8020, USA.
PMID: 20409709 DOI: 10.1016/j.bmcl.2010.03.086
Abstract

A series of 24-membered macrocyclic hexaoxazoles containing one or two aminoalkyl substituents was synthesized and evaluated for cytotoxicity and for their ability to selectively stabilize G-quadruplex DNA and RNA. The most cytotoxic analog 4a, with IC(50) values of 25 and 130 nM using KB3-1 and RPMI 8402 cells, is efficacious in vivo in athymic nude mice with a human tumor xenograft from the breast Cancer cell line MDA-MB-435.

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