6145-40-0Relevant academic research and scientific papers
Synthesis and biological activity of 2-anilino-4-(1H-pyrrol-3-yl) pyrimidine CDK inhibitors
Wang, Shudong,Wood, Gavin,Meades, Christopher,Griffiths, Gary,Midgley, Carol,McNae, Iain,McInnes, Campbell,Anderson, Sian,Jackson, Wayne,Mezna, Mokdad,Yuill, Rhoda,Walkinshaw, Malcolm,Fischer, Peter M.
, p. 4237 - 4240 (2004)
A series of 2-anilino-4-(1H-pyrrol-3-yl)pyrimidines were prepared and evaluated for their ability to inhibit cyclin-dependent kinases (CDKs). A number of analogues were found to be potent CDK2 and CDK4 inhibitors and to exhibit anti-proliferative activity
PYRIMIDINES, TRIAZINES AND THEIR USE AS PHARMACEUTICAL AGENTS
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Page/Page column 38, (2009/10/22)
A compound of formula (I) and its pharmaceutically acceptable salts or solvates and physiologically hydrolysable, solubilising or immobilisable derivatives wherein: Ar is a 5-membered heteroaryl ring wherein X1 and X2 are one or two
Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases
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, (2008/06/13)
The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative o thereof, wherein A, B, Ra, R1, R2, R3, and R4 are as described in the specification. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli; Lck and Src kinase. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
Cardiovascular activity of aromatic guanidine compounds.
Hughes et al.
, p. 1077,1080 (2007/10/04)
A series of aromatic guanidines and several 1-phenylbiguanides was prepared and tested for cardiovascular (CV) effects in anesthetized dogs measuring heart rate, blood pressure, carotid artery blood flow, and myocardial force changes. The predominant CV effect at minimally effective dose was vasoconstriction unassociated with cardiac stimulation. The structure-activity relationships of the compounds were discussed comparing their structural similarities to the beta-phenylethylamines. The most potent members of the series were phenylguanidines substituted in the 3 and 4 positions on the aromatic nucleus with hydroxy or chloro groups. Preliminary mechanism studies indicated that the 3,4-dihydroxyphenylguanidines act at least partially by a direct alpha-adrenergic mechanism
