122024-71-9

Upstream product

• 122024-75-3 C₁₆H₁₄O₃ 
• 14755-02-3 3-hydroxycinnamic acid 
• 100-39-0 benzyl bromide 
• 14755-02-3 3-hydroxy-trans-cinnamic acid 
• 122024-75-3 3-<3-(phenylmethoxy)phenyl>-2-propenoic acid 

Downstream Products

• 160383-26-6 3-chloro-5-(phenylmethoxy)benzothiophene-2-carboxamide 
• 1259977-93-9 methyl 5-(benzyloxy)-3-chlorobenzo[b]thiophene-2-carboxylate 
• 1259977-97-3 kb-NB₁₂₃-66 
• 1259978-05-6 Kb-NB₁₆₅-89 
• 1233533-04-4 kb-NB142-70 
• 172832-10-9 3,4-dihydro-9-methoxy[1]benzothieno[2,3-f]-1,4-thiazepin-5(2H)-one 
• 122024-51-5 5-Benzyloxy-3-isopropoxy-benzo[b]thiophene-2-carboxylic acid (1H-tetrazol-5-yl)-amide 
• 122024-80-0 5-Benzyloxy-3-isopropoxy-benzo[b]thiophene-2-carboxylic acid 

Relevant academic research and scientific papers

PROTEIN KINASE D INHIBITORS

Compounds according to Formula (I), are potent inhibitors of protein kinase D (pan-PKD) activity. PKD controls key signaling cascades in cells, affecting cell proliferation, gene transcription, and protein trafficking. Accordingly, pharmaceutically acceptable compositions of the inventive compounds are candidate therapeutics for pathological conditions conditioned by changes in PKD activity.

Synthesis and structure-activity relationships of benzothienothiazepinone inhibitors of protein kinase D

Protein kinase D (PKD) is a member of a novel family of serine/threonine kinases that regulate fundamental cellular processes. PKD is implicated in the pathogenesis of several diseases, including cancer. Progress in understanding the biological functions and therapeutic potential of PKD has been hampered by the lack of specific inhibitors. The benzoxoloazepinolone CID755673 was recently identified as the first potent and selective PKD inhibitor. The study of structure-activity relationships (SAR) of this lead compound led to further improvements in PKD1 potency. We describe herein the synthesis and biological evaluation of novel benzothienothiazepinone analogues. We achieved a 10-fold increase in the in vitro PKD1 inhibitory potency for the second generation lead kb-NB142-70 and accomplished a transition to an almost equally potent novel pyrimidine scaffold, while maintaining excellent target selectivity. These promising results will guide the design of pharmacological tools to dissect PKD function and pave the way for the development of potential anticancer agents.

Novel benzothiophene-, benzofuran-, and naphthalenecarboxamidotetrazoles as potential antiallergy agents

The synthesis and antiallergic activity of a series of novel benzothiophene-, benzofuran-, and naphthalenecarboxamidotetrazoles are described. A number of the compounds inhibit the release of histamine from anti-IgE stimulated basophils obtained from alle

Benzofurans and benzothiophenes having antiallergic activity and method of use thereof

Novel benzothiophenes having antiallergic activity and both novel and other selected benzothiophenes having activity for treating acute respiratory distress syndrome. The benzothiophenes of the present invention are particularly 2-tetrazolylcarboxamides of the benzothiophenes.