474686-33-4Relevant academic research and scientific papers
Macrocyclic hexaoxazoles: Influence of aminoalkyl substituents on RNA and DNA G-quadruplex stabilization and cytotoxicity
Satyanarayana, Mavurapu,Kim, Young-Ah,Rzuczek, Suzanne G.,Pilch, Daniel S.,Liu, Angela A.,Liu, Leroy F.,Rice, Joseph E.,LaVoie, Edmond J.
scheme or table, p. 3150 - 3154 (2010/09/10)
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 IC50 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.
THERAPEUTIC COMPOUNDS
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Page/Page column 25-26, (2009/07/03)
The invention provides compounds of formula I: wherein A, B, D, E, R1, R2, R3, R4, R5, X, and ----- have any values defined herein, as well as salts thereof. The compounds have activity as G-quadruplex DNA stabilizers and as anti-proliferative agents.
THERAPEUTIC COMPOUNDS
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Page/Page column 50-51, (2009/03/07)
The invention provides compounds of formula (I) wherein A, B, R1, F, G, n, n' and the dotted line have any values defined herein, as well as salts thereof. The compounds have activity as anti-proliferative agents.
THERAPEUTIC COMPOUNDS
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Page/Page column 36, (2008/06/13)
The invention provides compounds of formula I: wherein A, B, D, E, R1, R2, R3, R4, R5, X, and ----- have any values defined herein, as well as salts thereof. The compounds have activity as G-quadruplex DNA stabalizers and as anti-proliferative agents.
Regioselective synthesis of antiparallel loops on a macrocyclic scaffold constrained by oxazoles and thiazoles
Singh, Yogendra,Stoermer, Martin J.,Lucke, Andrew J.,Glenn, Matthew P.,Fairlie, David P.
, p. 3367 - 3370 (2007/10/03)
(matrix presented) The regioselective syntheses and structures are reported for two tris-macrocylic compounds, each possessing two antiparallel loops on a macrocyclic scaffold constrained by two oxazoles and two thiazoles. NMR solution structures show the
