6945-44-4Relevant academic research and scientific papers
HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS
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Paragraph 0216, (2021/01/23)
Heterocyclic compounds as CDK4 or CDK6 or other CDK inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Paragraph 0549-0551, (2019/04/25)
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Lewis Acid-Catalyzed Reductive Amination of Aldehydes and Ketones with N,N-Dimethylformamide as Dimethylamino Source, Reductant and Solvent
Yang, Luo,Lin, Jie,Kang, Lei,Zhou, Wang,Ma, Da-You
supporting information, p. 485 - 490 (2018/01/15)
A practical zinc acetate dihydrate-catalyzed reductive amination of various carbonyl compounds with N,N-dimethylformamide (DMF) as dimethylamino (Me2N) source, reductant and solvent has been developed. This reaction shows broad substrate scope,
BICYCLOANILINE DERIVATIVE
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Page/Page column 39, (2010/04/25)
The invention relates to a compound of a general formula (I): wherein A1 and A2 each mean a nitrogen atom or an optionally-substituted methine group; Ring B means a 5-membered to 7-membered aliphatic ring, or a spiro or bicyclo ring formed from the aliphatic ring and any other 3-membered to 7-membered aliphatic ring; R1 means a hydrogen atom, or an optionally-substituted C1-C6 alkyl group, or an optionally-substituted aryl, aralkyl or heteroaryl group; R2 means an optionally-substituted aryl, aralkyl or heteroaryl group; and X means a group of =NH or =O, etc. Based on its excellent Wee1 kinase-inhibitory effect, the compound of the invention has cell growth-inhibitory effect and has an additive/synergistic effect with any other anticancer agent, and is therefore useful in the field of medicine.
Synthesis, evaluation, and comparative molecular field analysis of 1- phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes as ligands for histamine H1 receptors
Bucholtz, Ehren C.,Brown, Randal L.,Tropsha, Alexander,Booth, Raymond G.,Wyrick, Steven D.
, p. 3041 - 3054 (2007/10/03)
A series of 1-phenyl-3-amino-1,2,3,4-tetrahydronaphthalenes (1-phenyl- 3-aminotetralins, PATs) previously was found to modulate tyrosine hydroxylase activity and dopamine synthesis in rodent forebrain through interaction with a binding site labeled by [3H]-(-)-(1R,3S)-trans-H2-PAT. Recently, we have discovered that PATs also bind with high affinity to the [3H]mepyramine- labeled H1 receptor in rat and guinea pig brain. Here, we report the synthesis and biological evaluation of additional PAT analogues in order to identify differences in binding at these two sites. Further molecular modifications involve the pendant phenyl ring as well as quaternary amine compounds. Comparison of about 38 PAT analogues, 10 structurally diverse H1 ligands, and several other CNS-active compounds revealed no significant differences in affinity at [3H]-(-)-trans-H2-PAT sites versus [3H]mepyramine-labeled H1 receptors. These results, together with previous autoradiographic brain receptor-mapping studies that indicate similar distribution of [3H]-(-)-trans-H2-PAT sites and [3H]mepyramine-labeled H1 receptors, suggest that both radioligands label the same histamine H1 receptors in rodent brain. We also report a revision of our previous comparative molecular field analysis (CoMFA) study of the PAT ligands that yields a highly predictive model for 66 compounds with a cross-validated R2 (q2) value of 0.67. This model will be useful for the prediction of high- affinity ligands at radiolabeled H1 receptors in mammalian brain.
Comparison of Biological Effects of N-Alkylated Congeners of β-Phenylethylamine Derived from 2-Aminotetralin, 2-Aminoindan, and 6-Aminobenzocycloheptene
Cannon, Joseph G.,Perez, Julio A.,Pease, Jonathan P,Long, John Paul,Flynn, Jan R.,et al.
, p. 745 - 749 (2007/10/02)
Three series of bicyclic, semirigid congeners of β-phenethylamine have been prepared for evaluation of the effect of ring size (and of concomitant conformational variation) on biological activity in a variety of assays for adrenergic and dopaminergic actions.Pharmacologic activity was associated with 2-aminotetralin and 2-aminoindan derivatives, but was not found with 6-aminobenzocycloheptene derivatives.Noteworthy is the ability of several aminotetralins and aminoindans to increase the hot-plate reaction time without eliciting dopaminergic effects.This action was not blocked by pretreatment with naloxone.
