Human telomerase inhibition by substituted acridine derivatives

A series of 3,6-disubstituted acridine derivatives have been rationally designed as telomerase inhibitors. They have been designed on the basis that inhibition of telomerase occurs by stabilising G-quadruplex structures formed by the folding of telomeric DNA. The most potent inhibitors have IC 50 va...

Celý popis

Uloženo v:

Podrobná bibliografie
Vydáno v:	Bioorganic & medicinal chemistry letters Ročník 9; číslo 17; s. 2463 - 2468
Hlavní autoři:	Harrison, R. John, Gowan, Sharon M., Kelland, Lloyd R., Neidle, Stephen
Médium:	Journal Article
Jazyk:	angličtina
Vydáno:	Oxford Elsevier Ltd 06.09.1999 Elsevier
Témata:	Acridines - chemistry Acridines - pharmacology Antineoplastic agents Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Biological and medical sciences Drug Screening Assays, Antitumor Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology General aspects Humans Medical sciences Pharmacology. Drug treatments Telomerase - antagonists & inhibitors Tumor Cells, Cultured Antineoplastic agent Human Enzyme Aminoamide Nitrogen heterocycle Transferases Acridine derivatives Enzyme inhibitor Cytotoxicity Tricyclic compound In vitro Ovary Nucleotidyltransferases Cell line Structure activity relation Tertiary amine Aromatic compound Chemical synthesis DNA-directed DNA polymerase
ISSN:	0960-894X, 1464-3405
On-line přístup:	Získat plný text
Tagy:	Přidat tag Žádné tagy, Buďte první, kdo vytvoří štítek k tomuto záznamu!

Popis
Shrnutí:	A series of 3,6-disubstituted acridine derivatives have been rationally designed as telomerase inhibitors. They have been designed on the basis that inhibition of telomerase occurs by stabilising G-quadruplex structures formed by the folding of telomeric DNA. The most potent inhibitors have IC 50 values against telomerase of between 1.3 and 8 μM, comparable to their cytotoxicity in ovarian cancer cell lines.
Bibliografie:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(99)00394-7