4778-99-8

Upstream product

• 6512-26-1 methyl 2,4-dimethoxy-6-(methoxycarbonylmethyl)benzoate 
• 71088-95-4 ethyl 5,7-dimethoxyindan-1-one-2-glyoxalate 
• 83375-20-6 2,4-dimethoxy-6-(methoxycarbonylmethyl)benzoic acid 
• 3686-57-5 2,4-dimethoxy-6-methylbenzoic acid 
• 616-38-6 carbonic acid dimethyl ester 
• 57749-86-7 ethyl 2,4-dimethoxy-6-methylbenzoate 
• 16909-11-8 3-(3,5-dimethoxyphenyl)acrylic acid 
• 7051-13-0 1-chloro-2,4-dimethoxybenzene 
• 6110-30-1 methyl <3,5-dihydroxy-2-(methoxycarbonyl)phenyl>acetate 
• 20767-04-8 (E)-3,5-dimethoxycinnamic acid 
• 717-94-2 3-(3,5-dimethoxyphenyl)propionic acid 
• 602278-05-7 (2-formyl-3,5-dimethoxy-phenyl)-acetic acid methyl ester 
• 6512-32-9 methyl 2-(3,5-dimethoxyphenyl)acetate 
• 877-88-3 3,5-dimethoxybenzyl bromide 

Downstream Products

• 6803-02-7 6-methoxymellein 
• 19314-92-2 3,4-dihydro-6,8-dihydroxy-3-methylisochromen-1-one 
• 1204-37-1 saccharonol A 
• 1702-86-9 8-hydroxy-6-methoxy-3-methylisocoumarin 
• 6512-26-1 methyl 2,4-dimethoxy-6-(methoxycarbonylmethyl)benzoate 
• 924300-55-0 3-(4-hydroxy-3,5-dimethyl-phenyl)-6,8-dimethoxy-isochromen-1-one 
• 1044871-80-8 3-(3,5-dimethyl-4-(2-(4-methylpiperazin-1-yl)ethoxy)phenyl)-6,8-dimethoxyisoquinolin-1(2H)-one 
• 1044872-19-6 3-[3,5-dimethyl-4-(2-(4-methyl piperazin-1-yl)-ethoxy)-phenyl]-6,8-dimethoxy-isochromen-1-one 
• 924300-54-9 acetic acid 4-(6,8-dimethoxy-1-oxo-1H-isochromen-3-yl)-2,6-dimethyl-phenyl ester 
• 924300-53-8 acetic acid 4-(6,8-dimethoxy-1,3-dioxo-isochroman-4-carbonyl)-2,6-dimethyl-phenyl ester 
• 924300-56-1 3-[4-(2-chloro-ethoxy)-3,5-dimethyl-phenyl]-6,8-dimethoxy-isochromen-1-one 
• 924300-57-2 3-[3,5-dimethyl-4-(2-morpholin-4-yl-ethoxy)-phenyl]-6,8-dimethoxy-isochromen-1-one 
• 1381876-80-7 6,8-dimethoxy-2-(4-methoxyphenyl)isoquinoline-1,3(2H,4H)-dione 
• 1381876-79-4 6,8-dimethoxy-2-(4-methylphenyl)isoquinoline-1,3(2H,4H)-dione 

Relevant academic research and scientific papers

Discovery of 2-aryl-8-hydroxy (or methoxy)-isoquinolin-1(2H)-ones as novel EGFR inhibitor by scaffold hopping

2-Aryl-8-hydroxy (or methoxy)-isoquinolin-1(2H)-one has been proposed as a novel scaffold of EGFR inhibitor based on scaffold hoping. In the present study, a series of 2-aryl-8-hydroxy (or methoxy)-isoquinolin-1(2H)-one derivatives were synthesized. Their antiproliferative activities in vitro were evaluated via MTT assay against two human cancer cell lines, including A431 and A549. The SAR of the title compounds was preliminarily discussed. The compounds with ideal inhibition were evaluated through ELISA-based EGFR-TK assay. Compound 6c showed the best activity against A431 and EGFR tyrosine kinase. These findings suggest that title compounds are EGFR inhibitors with novel structures.

Synthesis and antitumor activity evaluation of 2-arylisoquinoline-1,3(2H, 4H)-diones in vitro and in vivo

Six 2-(2-acylaminobenzothiazol-6-yl)isoquinoline-1,3(2H,4H)-diones (1a-1f) and five 2-arylisoquinoline-1,3(2H,4H)-diones (1g-1k) were synthesized by refluxing homophthalic anhydrides with 2-acylaminobenzothiazolyl-6-amine or substituted aniline in glacial acetic acid. The cytotoxic activities of 1a-1k were evaluated via MTT method against A431, A549, and PC3. Compound 1b relatively displayed a higher cytotoxic activity than the others. The antitumor effect of 1b were evaluated in established nude mice PANC-1 xenograft model. The results suggest that compound 1b could potentially inhibit tumor growth.

Total synthesis of viridicatumtoxin B and analogues thereof: Strategy evolution, structural revision, and biological evaluation

The details of the total synthesis of viridicatumtoxin B (1) are described. Initial synthetic strategies toward this intriguing tetracycline antibiotic resulted in the development of key alkylation and Lewis acid-mediated spirocyclization reactions to form the hindered EF spirojunction, as well as Michael-Dieckmann reactions to set the A and C rings. The use of an aromatic A-ring substrate, however, was found to be unsuitable for the introduction of the requisite hydroxyl groups at carbons 4a and 12a. Applying these previous tactics, we developed stepwise approaches to oxidize carbons 12a and 4a based on enol- and enolate-based oxidations, respectively, the latter of which was accomplished after systematic investigations that revealed critical reactivity patterns. The herein described synthetic strategy resulted in the total synthesis of viridicatumtoxin B (1), which, in turn, formed the basis for the revision of its originally assigned structure. The developed chemistry facilitated the synthesis of a series of viridicatumtoxin analogues, which were evaluated against Gram-positive and Gram-negative bacterial strains, including drug-resistant pathogens, revealing the first structure-activity relationships within this structural type.

TREATMENT OF DISEASES BY EPIGENETIC REGULATION

The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis.

COMPOUNDS FOR THE PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASES

The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.

PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF COMPLEX DISEASES AND THEIR DELIVERY BY INSERTABLE MEDICAL DEVICES

The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.

Total Synthesis of Premithramycinone H and Related Anthrapyran Antibiotics

Two approaches are described for the preparation of 2-(1',3'-dioxoalkyl)-substituted 1-hydroxyanthraquinones 10a-d and 20a-c, which were cyclized in a biomimetic-type reaction to the anthra[1,2-b]pyran skeletons 11a-d and 21a-c of the heydamcin- or pluram

An anionic polycondensation strategy for the synthesis of dibenzoxanthenones: Progress toward the synthesis of hypoxyxylerone

An anionic polycondensation has been used as the key step in a highly convergent strategy for the preparation of hypoxyxylerone derivatives.

Formal synthesis of angiogenesis inhibitor NM-3

We report the formal synthesis of angiogenesis inhibitor NM-3 (1) in six steps from either of the 2,4-dimethoxyhalobenzenes 13a,b or 3,5-dimethoxychlorobenzene (13c). The first key reaction is the regiospecific alkylation/rearrangement between the aryne derived from 13a-c with sodium diethylmalonate in THF to produce diester 11, which after hydrolysis and cyclization affords homophthalic anhydride 3. The second is the reaction of anhydride 3 with either ethyl 2-methylmalonate (28a), in the presence of 1,1′-carbonyldiimidazole, or ethyl-2-methylmalonyl chloride (28b) under basic conditions to afford key isocoumarin 27. The conversion of 27 constitutes a formal synthesis of NM-3.

An efficient synthesis of 3,5-dimethoxyhomophthalic acid, a key intermediate for synthesis of natural isocoumarins

3,5-Dimethoxyhomophthalic acid was prepared efficiently in three steps, from 3,5-dimethoxybenzyl bromide via rhodium-catalyzed direct carbonylation to 3,5-dimethoxyphenylacetic acid followed by successive o-formylation and oxidation. Isocoumarins related