956111-99-2Relevant academic research and scientific papers
A convenient method for synthesis of tetraoxazole peptide macrocycles
Zhang, Zhenjiang,Yuan, Gu
, p. 360 - 370 (2011/12/04)
G-quadruplex DNA plays important regulatory roles in the maintenance of telomere length and transcriptions inhibition of such oncogenes as c-myc, and thus has become an attractive target for the development of anti-cancer therapeutic agents. Poly-oxazole macrocycles are a promising new class of G-quadruplex binding ligands. Herein is described the synthesis of a tetraoxazole peptide macrocycle and an epimerization product. The synthetic unit was prepared by cyclization-oxidation of a diserine with one hydroxyl protected. Two-cycle coupling of the unit gave a linear tetraoxazole amide. The targeted molecule and the epimerization product were obtained after macrocyclization of the linear precursor and following removal of the protecting benzyl groups. With structural similarities to the most potent G-quadruplex stabilizer telomestatin, these two molecules might potentially be used to probe the biological significance of G-quadruplex' in vivo.
THERAPEUTIC COMPOUNDS
-
, (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
-
Page/Page column 30, (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.
Novel polyoxazole-based cyclopeptides from Streptomyces sp. Total synthesis of the cyclopeptide YM-216391 and synthetic studies towards telomestatin
Deeley, Jon,Bertram, Anna,Pattenden, Gerald
supporting information; experimental part, p. 1994 - 2010 (2009/01/31)
A convergent, complementary, synthetic approach to the contiguously linked tris-oxazole units 10, 11 and 12 in telomestatin (1) and YM-216391 (2) is described. The route involves coupling reactions between oxazole 4-carboxylic acids, viz16a, 16c, 16d and
THERAPEUTIC COMPOUNDS
-
Page/Page column 47, (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.
