91099-19-3

Upstream product

• 536-90-3 m-Anisidine 
• 122-04-3 4-nitro-benzoyl chloride 
• 139-77-5 1-(3-methoxyphenyl)urea 
• 62-23-7 4-nitro-benzoic acid 

Downstream Products

• 247080-14-4 N-(3-methoxyphenyl)-4-nitrobenzene-1-carbothioamide 
• 169947-07-3 4-acetylamino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-methoxyphenyl)benzamide 
• 169946-76-3 4-amino-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-methoxyphenyl)benzamide 
• 169946-29-6 4-nitro-N-{2-[4-(4-fluorobenzoyl)piperidino]ethyl}-N-(3-methoxyphenyl)benzamide 
• 247080-35-9 2-(4-amino-3-iodophenyl)-5-methoxybenzothiazole 
• 247080-37-1 2-(4-amino-3-chloro-phenyl)-benzothiazol-5-ol 
• 247080-53-1 2-(4-amino-3-chlorophenyl)-5-methoxybenzothiazole 
• 1149760-92-8 7-methoxy-2-(4-nitrophenyl)-1,3-benzothiazole 
• 162374-51-8 5-hydroxy-2-(4-aminophenyl)-1,3-benzothiazole 
• 162374-46-1 5-methoxy-2-(4-nitrophenyl)-1,3-benzothiazole 
• 162374-77-8 5-methoxy-2-(4-aminophenyl)-1,3-benzothiazole 

Relevant academic research and scientific papers

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.

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).

The flocculated acryloyldimethyltauric molecule ligand

Provided are certain benzothiazole, imidazothiazole, imidazopyrimidine and imidazopyridine compounds, including, for example: formula (I) and pharmaceutically and physiologically acceptable salts, hydrates, and solvates thereof. Such compounds can be used as diagnostic ligands or labels of tau protein and PHF.

Synthesis of 2-(4-aminophenyl) benzothiazole derivatives and use thereof

The present invention provides a method of preparing a compound of formula 6 comprising: (a) reacting a compound of formula 1 with a compound of formula 2 to form a compound of formula 3 wherein X of formula 2 is Cl or OH; (b) treating the compound formula 3 with Lawesson's reagent to form a compound of formula 4 (c) reacting a compound of formula 4 with potassium ferricyanide to produce a compound of formula 5 and (d) performing catalytic reduction of nitro group of the compound of formula 5 with palladium on charcoal to generate the compound of formula 6, wherein R1 of formulae 1-6 is H, C1-10 alkyl, C1-10 alkoxy or C1-10 haloalkyl, and R2 of formulae 1-6 is H or C1-10 alkyl. The present invention also provides a photodynamic therapy to a patient having at least one tumor comprising the steps of: administering a compound of formula 6 (wherein R1 and R2 are defined as the above) in a pharmaceutically acceptable carrier to the patient; waiting for a sufficient time to allow the administered compound to be taken up by a target tissue having the at least one tumor; and irradiating a region of the patient containing the target tissue; wherein growth of the tumor is inhibited.

SYNTHESIS OF 2-(4-AMINOPHENYL) BENZOTHIAZOLE DERIVATIVES AND USE THEREOF

The present invention provides a method of preparing a compound of formula 6 comprising: (a) reacting a compound of formula 1 with a compound of formula 2 to form a compound of formula 3 wherein X of formula 2 is Cl or OH; (b) treating the compound formula 3 with Lawesson's reagent to form a compound of formula 4 (c) reacting a compound of formula 4 with potassium ferricyanide to produce a compound of formula 5 and (d) performing catalytic reduction of nitro group of the compound of formula 5 with palladium on charcoal to generate the compound of formula 6, wherein R1 of formulae 1-6 is H, C1-10 alkyl, C1-10 alkoxy or C1-10 haloalkyl, and R2 of formulae 1-6 is H or C1-10 alkyl. The present invention also provides a photodynamic therapy to a patient having at least one tumor comprising the steps of: administering a compound of formula 6 (wherein R1 and R2 are defined as the above) in a pharmaceutically acceptable carrier to the patient; waiting for a sufficient time to allow the administered compound to be taken up by a target tissue having the at least one tumor; and irradiating a region of the patient containing the target tissue; wherein growth of the tumor is inhibited.

Synthesis, and biological evaluation of 2-(4-aminophenyl)benzothiazole derivatives as photosensitizing agents

Photodynamic therapy (PDT) employing exogenous photosensitizers is currently being approved for treatment of basal cell carcinoma (BCC). 2-(4-Aminophenyl)benzothiazoles (6) consist of chromophoric structure and absorb light in the UVA (315-400 nm). These results encouraged us to design and synthesize a diversity of 2-phenylbenzothiazoles (6). Studies on the apoptotic mechanism involved in photosensitive effects induced by UVA-activated 6 in BCC cells are carried out in the present article. 6-UVA-treated cells displayed several features of apoptosis, including an increase in the sub-G1 population, a significantly increased annexin V binding, and activation of caspase-3. 6-UVA induced a decrease in mitochondrial membrane potential (Δψ mt) and ATP via enhanced ROS generation and promoted phosphorylation of extracellular signal-regulated kinase (ERK) and p38 MAPK expression. These results suggest that 6-UVA elicits photosensitive effects in mitochondria processes which involve ERK and p38 activation, and ultimately lead to BCC cell apoptosis.

Antitumor benzothiazoles. 8.1 Synthesis, metabolic formation, and biological properties of the C- and N-oxidation products of antitumor 2-(4- aminophenyl)-benzothiazoles

2-(4-Aminophenyl)benzothiazoles 1 and their N-acetylated forms have been converted to C and N-hydroxylated derivatives to investigate the role of metabolic oxidation in the mode of action of this series of compounds. 2-(4- Amino-3-methylphenyl)benzothiazole (1a, DF 203, NSC 674495) is a novel and potent antitumor agent with selective growth inhibitory properties against human cancer cell lines. Very low IC50 values (14C]1a derived radioactivity was observed in the sensitive MCF-7 cell line but not in the insensitive MDA-MB-435 cell line. The mechanism of growth inhibition by 1a, which is unknown, may be dependent on the differential metabolism of the drug to an activated form by sensitive cell lines only and its covalent binding to an intracellular protein. However, the 6-hydroxy derivative 6c is not the 'active' metabolite since, like all other C- and N-hydroxylated benzothiazoles examined in this study, it is devoid of antitumor properties in vitro.

Substituted cyclic amine compound, production process thereof and pharmaceutical composition for circulatory organ use containing the same

A substituted cyclic amine compound represented by the following general formula (1) STR1 wherein each of R1 to R5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or the like, A represents a carbonyl group or a sulfonyl group, B represents a methine moiety or a nitrogen atom, D represents a methine moiety, a nitrogen atom or =N(→O)-- and n is an integer of 2 to 3; and synthetic methods thereof. The inventive compound is useful in preventing and treating circulatory organ-related diseases such as hypertension, ischemic heart disease, cerebrovascular disease, peripheral circulatory disease and the like.

Central Nervous System Active Compounds. XIV On the Cyclization of N-Acyl-N'-arylureas

The cyclization of N-acyl-N'-arylureas in polyphosphoric acid has been reinvestigated.The product is not only the 4-substituted quinazolin-2(1H)-one as reported, but also contains the 2-acylaniline in major proportions.Two minor products have also been isolated.At 80 deg, an intermediate has been detected, the properties of which are consistent with it being the corresponding 2-acylphenylurea.Acyl ureas with strongly electron-withdrawing acyl groups from major amount of the corresponding anilide by the formal loss of cyanic acid.The application of this reaction tothe synthesis of quinazolinylphthalides has been investigated.