172832-10-9

Upstream product

• 41280-81-3 methyl 3-chloro-5-methoxybenzo[b]thiophene-2-carboxylate 
• 156-57-0 2-mercaptoethylamine hydrochloride 
• 60-23-1 Cysteamine 
• 122024-75-3 C₁₆H₁₄O₃ 
• 1259977-93-9 methyl 5-(benzyloxy)-3-chlorobenzo[b]thiophene-2-carboxylate 
• 1259977-97-3 kb-NB₁₂₃-66 
• 1233533-04-4 kb-NB142-70 
• 74-88-4 methyl iodide 
• 14755-02-3 3-hydroxycinnamic acid 
• 122024-71-9 3-Chloro-5-(phenylmethoxy)-benzo[b]thiophene-2-carbonyl chloride 
• 122024-75-3 3-<3-(phenylmethoxy)phenyl>-2-propenoic acid 
• 14755-02-3 3-hydroxy-trans-cinnamic 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.

Benzothiophene inhibitors of MK2. Part 1: Structure-activity relationships, assessments of selectivity and cellular potency

Identification of potent benzothiophene inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK2), structure-activity relationship (SAR) studies, selectivity assessments against CDK2, cellular potency and mechanism of action are pres

Novel benzthiodiazepinones as antiherpetic agents: SAR improvement of therapeutic index by alterations of the seven-membered ring

A series of novel benzthiodiazepinones was studied as antiherpetic agents. Significant improvements in potency and therapeutic index in a viral replication assay were realized over the starting molecule. The role of stereospecific substitution on the diazepine ring and optimal nitrogen substitution were investigated.

Methods for inhibiting and controlling viral growth

Benzothiophene, benzofuran and indolethiazepinones, oxazepinones, and diazepinones are effective therapeutic agents for treating viral diseases, including those caused by herpesvirus and HIV.

Method for treating inflammatory disease in humans

Benzothiophene, benzofuran and indole-thiazepinones, oxazepinones and diazepinones as well as methods of preparation thereof are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases.