24730-11-8

Upstream product

• 104-94-9 4-methoxy-aniline 
• 122-04-3 4-nitro-benzoyl chloride 
• 3128-43-6 S-phenyl 4-nitrobenzothioate 
• 6631-86-3 S-(p-chlorophenyl) p-nitrothiobenzoate 
• 28122-84-1 4-nitrothiobenzoic acid S-p-tolyl ester 
• 69737-96-8 S-(p-nitrophenyl) p-nitrothiobenzoate 
• 696-62-8 para-iodoanisole 
• 619-80-7 4-nitrobenzamide 
• 623-73-4 diazoacetic acid ethyl ester 
• 5455-87-8 4-methoxy-N-(4-nitrobenzylidene)aniline 
• 62-23-7 4-nitro-benzoic acid 
• 636-98-6 p-nitrobenzene iodide 
• 201230-82-2 carbon monoxide 
• 555-16-8 4-nitrobenzaldehdye 

Downstream Products

• 313497-47-1 4-nitro-benzoic acid-(4-methoxy-2-nitro-anilide) 
• 29955-50-8 N-(p-anisyl)-4-nitrobenzenecarboxyimidoyl chloride 
• 73702-95-1 N-(4-methoxyphenyl)-4-nitrothiobenzamide 
• 43036-17-5 2-(4-aminophenyl)-6-methoxybenzothiazole 
• 43036-14-2 6-methoxy-2-(4-nitrophenyl)benzothiazole 
• 178804-18-7 2-(4’-aminophenyl)-6-hydroxybenzothiazole 
• 480391-86-4 6-hydroxy-2-(4'-nitrophenyl)-1,3-benzothiazole 
• 566170-03-4 2-(4′-aminophenyl)-6-methoxymethoxybenzothiazole 
• 566170-02-3 6-methoxymethoxy-2-(4'-nitrophenyl)-1,3-benzothiazole 
• 1447816-85-4 4-[(1,1-dioxidobenzo[d]isothiazol-3-yl)amino]-N-(4-methoxyphenyl)benzamide 
• 1509916-05-5 tri-tert-butyl 2,2',2''-(10-(2-((6-((4-(6-methoxybenzo[d]thiazol-2-yl)phenyl)amino)6-oxohexyl)amino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetate 
• 1509916-10-2 2,2',2''-(10-(2-((6-((4-(6-methoxybenzo[d]thiazol-2-yl)phenyl)amino)-6-oxohexyl)amino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetic acid 
• 1509916-06-6 4-(2-chloroacetamido)-N-(4-(6-methoxybenzo[d]thiazol-2-yl)phenyl)benzamide 
• 1509916-07-7 tri-tert-butyl 2,2',2''-(((10-(2-((4-(6-methoxybenzo[d]thiazol-2-yl)phenyl)carbamoyl)phenyl)amino)-2-oxoethyl)-1,4,7,10-tetraazacyclododecane-1,4,7-triyl)triacetate 

Relevant academic research and scientific papers

Design, synthesis and biological evaluation of novel 2-phenyl pyrimidine derivatives as potent Bruton's tyrosine kinase (BTK) inhibitors

BTK is an effective target for the treatment of B-cell malignant tumors and autoimmune diseases. In this work, a series of 2-phenyl pyrimidine derivatives were prepared and their preliminary in vitro activities on B-cell leukemia cells as well as the BTK enzyme were determined. The results showed that compound 11g displayed the best inhibitory activity on BTK with an inhibition rate of 82.76% at 100 nM and excellent anti-proliferation activity on three B-cell leukemia lines (IC50 = 3.66 μM, 6.98 μM, and 5.39 μM against HL60, Raji and Ramos, respectively). Besides, the flow cytometry analysis results indicated that 11g inhibited the proliferation of the Raji cells in a dose- and time-dependent manner, and blocked the Ramos cells at the G0/G1 phase, which is in accordance with the positive control ibrutinib. The mechanism investigation demonstrated that 11g could inhibit the phosphorylation of BTK and its downstream substrate phospholipase γ2 (PLCγ2). All these results showed that 11g was a promising lead compound that merited further optimization as a novel class of BTK inhibitor for the treatment of B-cell lymphoblastic leukemia.

Identification of new pyrrolo[2,3-d]pyrimidines as potent VEGFR-2 tyrosine kinase inhibitors: Design, synthesis, biological evaluation and molecular modeling

Vascular endothelial growth factor receptor-2 (VEGFR-2) plays a crucial role in cancer angiogenesis. In the current study, a series of novel pyrrolo[2,3-d]pyrimidine based-compounds was designed and synthesized as VEGFR-2 inhibitors, in accordance to the structure activity relationship (SAR) studies of known type II VEGFR-2 inhibitors. The newly synthesized compounds were evaluated for their ability to inhibit VEGFR-2 kinase enzyme in vitro. All the tested compounds demonstrated highly potent dose-related VEGFR-2 inhibition with IC50 values in nanomolar range. Among these compounds, pyrrolo[2,3-d]pyrimidine derivatives carrying biaryl urea moieties (12d and 15c) exhibited IC50 values of 11.9 and 13.6 nM respectively. Additionally, most of the newly synthesized final compounds were tested on 60 human cancer cell lines. Docking of these compounds into the inactive conformation of VEGFR-2 was performed which showed comparable binding modes to that of the FDA approved VEGFR-2 kinase inhibitors. These newly discovered potent kinase inhibitors could be considered as potential candidates for the development of new targeted anticancer agent.

A convenient one-pot synthesis of: N -substituted amidoximes and their application toward 1,2,4-oxadiazol-5-ones

The first direct one-pot approach for the synthesis of N-substituted amidoximes from secondary amides or the intermediate amides has been developed. Through the Ph3P-I2-mediated dehydrative condensation, a variety of N-aryl and N-alkyl amidoximes (R1(CNOH)NHR2, where R1 or R2 = aryl, alkyl, or benzyl) were readily afforded under mild conditions and short reaction times. The synthetic application of the obtained amidoximes has also been demonstrated through the formation of 1,2,4-oxadiazolones via base-mediated carbonylative cyclization with 1,1′-carbonyldiimidazole.

2-phenylpyrimidine compounds, preparation method and medical application

The invention belongs to the field of medicines and particularly relates to 2-phenylpyrimidine compounds and pharmacologically-acceptable salts thereof and an isotope marker. The invention also discloses a pharmaceutical composition containing the substances and application of the pharmaceutical composition for treating diseases related with protein kinase activity, such as cancer and inflammation. (The formula is shown in the description).

Synthesis and biological evaluation of cis-restricted triazole/tetrazole mimics of combretastatin-benzothiazole hybrids as tubulin polymerization inhibitors and apoptosis inducers

A series of colchicine site binding tubulin inhibitors were synthesized by the modification of the combretastatin pharmacophore. The ring B was replaced by the pharmacologically relevant benzothiazole scaffolds, and the cis configuration of the olefinic b

2-Arylaminobenzothiazole-arylpropenone conjugates as tubulin polymerization inhibitors

A new series of 2-arylaminobenzothiazole-arylpropenone conjugates 5-6(a-r) was designed, synthesized and investigated for their cytotoxic potency against the various human cancer cell lines. Most of these conjugates exhibited cytotoxic activity and inhibi

Poly(methylhydrosiloxane) as a green reducing agent in organophosphorus-catalysed amide bond formation

Development of catalytic amide bond formation reactions has been the subject of the intensive investigations in the past decade. Herein we report an efficient organophosphorus-catalysed amidation reaction between unactivated carboxylic acids and amines. Poly(methylhydrosiloxane), a waste product of the silicon industry, is used as an inexpensive and green reducing agent for in situ reduction of phosphine oxide to phosphine. The reported method enables the synthesis of a wide range of secondary and tertiary amides in very good to excellent yields.

Design, synthesis and antimetastatic evaluation of 1-benzothiazolylphenylbenzotriazoles for photodynamic therapy in oral cancer cells

We have designed and synthesized a new series of 1-benzothiazolylphenylbenzotriazoles 9a-p and studied their antimetastatic mechanism involved in photosensitive effects induced by UVA in oral cancer cell Ca9-22. Our results revealed that the compounds plus UVA significantly suppressed migration and invasion, as detected by wound healing assay and Boyden chamber assay. Quantitative RT-PCR assay indicated that compound 9i plus UVA induced an antimetastatic effect through up-regulation of syndecan-1 and TIMP-3 and down-regulation of heparanase, MMP-2 and MMP-9 mRNA expressions. Western blot analysis showed that Ca9-22 treated with 9i plus UVA resulted in decreased levels of p-EGFR and p-ERK, MMP-2 and MMP-9, and an increased level of TIMP-3. These results are the first to report the function of UVA-activated 1-benzothiazolylphenylbenzotriazoles in tumor metastasis and their underlying molecular mechanism, and thus suggest that compound 9i plus PDT may serve as a potential ancillary modality for the treatment of oral cancer.

Stable and Reusable Binaphthyl-Supported Palladium Catalyst for Aminocarbonylation of Aryl Iodides

A binaphthyl-supported Pd nanoparticles (Pd-BNP)-catalyzed aminocarbonylation of aryl iodides in the presence of carbon monoxide and amines for the synthesis of amides has been developed. This methodology provides an efficient route for the synthesis of a COX-2 enzyme inhibitor having anti-inflammatory activity.

Efficient conversion of acids and esters to amides and transamidation of primary amides using OSU-6

OSU-6, an MCM-41 type hexagonal mesoporous silica with strong Bronsted acid properties, has been used to promote the high-yield conversion of carboxylic acids and esters to carboxamides as well as transamidations of primary amides in a one-pot solventless approach. A metal-free heterogeneous catalyst that promotes all of these processes has not been previously reported. OSU-6 enables these transformations to proceed in shorter times and at lower temperatures for a broad range of substrates. An added benefit is that the catalyst can be recycled and reused multiple times without significant loss of activity.