CDK2 inhibitors have been proposed as effective anti‐cancer therapeutics. We show here
that CYC202 (R‐roscovitine) is a potent inhibitor of recombinant CDK2/cyclin E kinase activity …

The main difficulty in the development of ATP antagonist kinase inhibitors is target specificity,
since the ATP-binding motif is present in many proteins. We introduce a strategy that has …

Through cell-based screening of our kinase-directed compound collection, we discovered
that a subset of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amines were potent cytotoxic agents …

A family of 4-heteroaryl-2-amino-pyrimidine CDK2 inhibitor lead compounds was discovered
with the new database-mining program LIDAEUS through in silico screening. Four …

… Of the total radioactivity, 95% was recovered within the first 24 h (data from McClue and
Stuart, article in preparation). The tissue distribution and metabolism of roscovitine (seliciclib) in …

R-roscovitine (seliciclib, CYC202) is a cyclin-dependent kinase inhibitor currently in phase II
clinical trials in patients with cancer. Here, we describe its mouse metabolism and …

We have investigated the effects of in vivo lithium treatment on cerebral inositol phospholipid
metabolism. Twice‐daily treatment of rats with LiCl (3 mEq/kg) for 3 or 16 days resulted in a …

The alpha 2-C10 adrenergic receptor from human platelets was expressed permanently in
Rat-1 fibroblasts. A series of clones that varied in expression of the receptor from 0 to 3.5 pmol…

Seliciclib (R-roscovitine, CYC202) is a small molecule inhibitor of cyclin-dependent kinases
currently in phase II clinical trials as an anticancer agent. We examined the metabolism of …

The cyclin-dependent kinase inhibitor (R)-2-(6-benzylamino-9-isopropyl-9H-purin-2-ylamino)butan-1-ol
(roscovitine, 1a), as well as its (S)-enantiomer 1b, were synthesised. The …