161006-18-4

Upstream product

• 18162-48-6 tert-butyldimethylsilyl chloride 
• 108-46-3 recorcinol 
• 288-32-4 1H-imidazole 
• 1067665-43-3 (3-benzyloxy-phenoxy)-tert-butyl-dimethyl-silane 
• 1114567-56-4 1-(tert-butyldimethylsilyloxy)-3-(tert-butyldiphenylsilyloxy)benzene 

Downstream Products

• 172832-33-6 3-(tert-Butyl-dimethyl-silanyloxymethyl)-6-[3-(tert-butyl-dimethyl-silanyloxy)-phenoxymethyl]-[1,2]dithiine 
• 865541-56-6 2-[4-(tert-butyl-dimethyl-silyloxy)-2-hydroxy-phenylsulfanyl]-isoindole-1,3-dione 
• 850663-85-3 3-{[2-(4-amino-furazan-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-6-yl]oxy}phenol 
• 1092494-91-1 C₂₃H₃₁BrO₄Si 
• 1178513-82-0 (2-bromophenyl)(tert-butyl)(3-(tert-butyldimethylsilyloxy)phenoxy)(phenyl)silane 
• 129742-35-4 4-[(tert-butyldimethylsilyl)oxy]-2-hydroxybenzaldehyde 
• 1227735-37-6 C₂₄H₃₇BrO₃Si₂ 
• 65250-71-7 3-((4-chlorobenzyl)oxy)phenol 
• 165390-74-9 3-(3-methoxy-benzyloxy)-phenol 
• 1569070-15-0 C₂₇H₂₃N₃O₄S*ClH 
• 1569070-19-4 C₃₁H₂₅N₃O₄*ClH 
• 1569070-93-4 C₂₀H₂₅NO₂Si 

Relevant academic research and scientific papers

Structure-aided optimization of non-nucleoside M. tuberculosis thymidylate kinase inhibitors

Mycobacterium tuberculosis thymidylate kinase (MtTMPK) has emerged as an attractive target for rational drug design. We recently investigated new families of non-nucleoside MtTMPK inhibitors in an effort to diversify MtTMPK inhibitor chemical space. We here report a new series of MtTMPK inhibitors by combining the Topliss scheme with rational drug design approaches, fueled by two co-crystal structures of MtTMPK in complex with developed inhibitors. These efforts furnished the most potent MtTMPK inhibitors in our assay, with two analogues displaying low micromolar MIC values against H37Rv Mtb. Prepared inhibitors address new sub-sites in the MtTMPK nucleotide binding pocket, thereby offering new insights into its druggability. We studied the role of efflux pumps as well as the impact of cell wall permeabilizers for selected compounds to potentially provide an explanation for the lack of correlation between potent enzyme inhibition and whole-cell activity.

Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1

G-protein-coupled receptors (GPCRs) are the molecular target of 40% of marketed drugs and the most investigated structures to develop novel therapeutics. Different members of the GPCRs superfamily can modulate the same cellular process acting on diverse pathways, thus representing an attractive opportunity to achieve multitarget drugs with synergic pharmacological effects. Here, we present a series of compounds with dual activity toward cysteinyl leukotriene receptor 1 (CysLT1R) and G-protein-coupled bile acid receptor 1 (GPBAR1). They are derivatives of REV5901-the first reported dual compound-with therapeutic potential in the treatment of colitis and other inflammatory processes. We report the binding mode of the most active compounds in the two GPCRs, revealing unprecedented structural basis for future drug design studies, including the presence of a polar group opportunely spaced from an aromatic ring in the ligand to interact with Arg792.60 of CysLT1R and achieve dual activity.

Gold(I)-Catalyzed Intramolecular Hydroarylation of Phenol-Derived Propiolates and Certain Related Ethers as a Route to Selectively Functionalized Coumarins and 2 H-Chromenes

Methods are reported for the efficient assembly of a series of phenol-derived propiolates, including the parent system 56, and their Au(I)-catalyzed cyclization (intramolecular hydroarylation) to give the corresponding coumarins (e.g., 1). Simple syntheses of natural products such as ayapin (144) and scoparone (145) have been realized by such means, and the first of these subject to single-crystal X-ray analysis. A related process is described for the conversion of propargyl ethers such as 156 into the isomeric 2H-chromene precocene I (159), a naturally occurring inhibitor of juvenile hormone biosynthesis.

Acid-Promoted Cascade Cyclization to Produce 2-(4′-Alkoxyaryl)-3,4-Fused Tricyclic Dihydrobenzopyrans via a Vinylidene para-Quinone Methide Intermediate

We developed a novel method for synthesizing 2-(4-hydroxyaryl)-3,4-fused tricyclic dihydrobenzopyrans with 2,3-syn and 3,4-syn motif based on the acid-promoted cascade cyclization via vinylidene para-quinone methide intermediates. Using easily prepared li

BROMODOMAIN INHIBITORS FOR TREATING DISEASE

Disclosed herein are compounds and compositions useful in the treatment of bromodomain-containing protein-mediated diseases, such as cancer, having the structure of Formula I: Methods of inhibiting activity of a bromodomain-containing protein in a human or animal subject are also provided.

Total synthesis of the 2-arylbenzo[b]furan-containing natural products from Artocarpus

In this study, 2-arylbenzo[b]furan-containing derivatives moracin C (1) and moracin M (4), the natural products from Artocarpus, have been synthesized in highest overall yield to date (1, 7 steps with an overall yield of 41.9%; 4, 6 steps with an overall yield of 56.3%), and we also report the first total synthesis of artoindonesianin B-1 (2), another member of this family, in the same route (8 steps with an overall yield of 11.3%). This discovery provides a concise route for preparing enough amounts of 1, 2, and 4 as well as 2-arylbenzo[b]furan-containing natural product-like analogs (71-74) to explore the biological potential.

SECONDARY AMINES AS THERAPEUTIC AGENTS

Compounds such as those represented by Formulas 1-6 can be used in topical liquids, creams, or other dosage forms such as solids, for reducing intraocular pressure, treating glaucoma, growing hair, or other medical uses.

PROTEIN KINASE INHIBITORS

The present invention relates to a novel family of inhibitors of protein kinases. In particular, the present invention relates to inhibitors of the members of the Tec and Src protein kinase families.

PROTEIN KINASE INHIBITORS

The present invention relates to a novel family of inhibitors o f protein kinase of formula 1 and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src and Btk protein kinase families

PROTEIN KINASE INHIBITORS

The present invention relates to a novel family of inhibitors of protein kinases. In particular, the present invention relates to inhibitors of the members of the Tec and Src protein kinase families, more particularly Btk, having the general formula (1): A-Y-E-W-Z (1.)