J 2012

Cyclin-dependent kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres

JORDA, Radek; Kamil PARUCH a Vladimír KRYŠTOF

Základní údaje

Originální název

Cyclin-dependent kinase Inhibitors Inspired by Roscovitine: Purine Bioisosteres

Autoři

JORDA, Radek; Kamil PARUCH a Vladimír KRYŠTOF

Vydání

CURRENT PHARMACEUTICAL DESIGN, SHARJAH, BENTHAM SCIENCE PUBL LTD, 2012, 1381-6128

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

10401 Organic chemistry

Stát vydavatele

Spojené arabské emiráty

Utajení

není předmětem státního či obchodního tajemství

Impakt faktor

Impact factor: 3.311

Označené pro přenos do RIV

Ano

Kód RIV

RIV/00216224:14310/12:00062050

Organizační jednotka

Přírodovědecká fakulta

UT WoS

Klíčová slova anglicky

Cancer; cyclin-dependent kinase; inhibitor; roscovitine; bioisostere

Štítky

Změněno: 9. 4. 2013 18:43, Ing. Andrea Mikešková

Anotace

V originále

Roscovitine is a synthetic inhibitor of cyclin-dependent kinases that is currently undergoing clinical trials as a candidate drug for some oncological indications. Its discovery prompted many research teams to further optimize its structure or to initiate their own related but independent studies. This article reviews known roscovitine bioisosteres that have been prepared as CDK inhibitors using different core heterocycles. The individual bioisostere types have been described and explored to a different extent, which complicates direct comparisons of their biochemical activity - only six direct analogs containing different purine bioisosteres have been prepared and evaluated side by side with roscovitine. Only four types of bioisosteres have demonstrated improved biological properties, namely pyrazolo[1,5-a]-1,3,5-triazines, pyrazolo[1,5-a]pyrimidines, pyrazolo[1,5-a]pyridines and pyrazolo[4,3-d] pyrimidines.