24805-50-3

Upstream product

• 331-25-9 (3-fluorophenyl)acetic acid 
• 7292-74-2 DL-2-(3-fluorophenyl)glycine 

Downstream Products

• 251366-58-2 α-bromo-(3-fluorophenyl)acetamide 
• 251366-32-2 2-bromo-2-(p-fluorophenyl)acetamide 
• 151295-24-8 9-Chloro-8-fluoro-2-(3-fluoro-phenyl)-6-oxo-2,3-dihydro-6H-1-thia-3a-aza-phenalene-5-carboxylic acid ethyl ester 
• 151295-17-9 8-Chloro-7-fluoro-2-(3-fluoro-phenyl)-4H-benzo[1,4]thiazin-3-one 
• 151295-20-4 8-Chloro-7-fluoro-2-(3-fluoro-phenyl)-3,4-dihydro-2H-benzo[1,4]thiazine 
• 151295-14-6 (2-Chloro-3-fluoro-6-nitro-phenylsulfanyl)-(3-fluoro-phenyl)-acetic acid 

Relevant academic research and scientific papers

Phthalimide compound as well as preparation method and application thereof

The invention provides a phthalimide compound or a pharmaceutically acceptable salt thereof, wherein the structure of the phthalimide compound is shown as a formula I; in the formula I, R1 is selected from hydrogen, aliphatic hydrocarbon, alkoxy and halogen; R2 and R3 are the same or different and are selected from hydrogen, aliphatic hydrocarbon, alkoxy and halogen; or R2, R3 and connected N atoms are cyclized to form a closed substituted or unsubstituted five-membered or six-membered ring; R1, R2 and R3 can be unsubstituted or substituted by straight chain or branched chain alkyl or alkoxy selected from C1 - C10 and halogen; and R1, R2 and R3 are not hydrogen at the same time. The compound disclosed by the invention has the effect of a ROCK inhibitor and an anti-tumor effect, and is expected to be used as a clinical medicine with a relatively high therapeutic index.

Benzoxazinone-containing 3,5-dimethylisoxazole derivatives as BET bromodomain inhibitors for treatment of castration-resistant prostate cancer

The bromodomain and extra-terminal proteins (BET) have emerged as promising therapeutic targets for the treatment of castration-resistant prostate cancer (CRPC). We report the design, synthesis and evaluation of a new series of benzoxazinone-containing 3,5-dimethylisoxazole derivatives as selective BET inhibitors. One of the new compounds, (R)-12 (Y02234), binds to BRD4(1) with a Kd value of 110 nM and blocks bromodomain and acetyl lysine interactions with an IC50 value of 100 nM. It also exhibits selectivity for BET over non-BET bromodomain proteins and demonstrates reasonable anti-proliferation and colony formation inhibition effect in prostate cancer cell lines such as 22Rv1 and C4-2B. The BRD4 inhibitor (R)-12 also significantly suppresses the expression of ERG, Myc and AR target gene PSA at the mRNA level in prostate cancer cells. Treatment with (R)-12 significantly suppresses the tumor growth of prostate cancer (TGI = 70%) in a 22Rv1-derived xenograft model. These data suggest that compound (R)-12 is a promising lead compound for the development of a new class of therapeutics for the treatment of CRPC.

Catalytic Asymmetric Conjugate Addition and Sulfenylation of Diarylthiazolidin-2,4-diones

This work reports the first application of diarylthiazolidin-2,4-diones as nucleophiles in asymmetric catalysis. By utilizing chiral amino acid-based (thio)urea-tertiary amines as the catalysts, we successively established asymmetric conjugate addition to nitroolefins and sulfenylation to N-(sulfanyl)-succinimides of diarylthiazolidin-2,4-diones. Two series of biologically important 5-aryl-5-substituted thiazolidin-2,4-diones were obtained with high enantio- and diastereoselectivities (up to >99% ee and >19:1 dr). The enantioenriched adducts were found to show satisfactory anticancer activities against three different cancer cell lines using the MTT assay. All of these successes depended on the development of a general and expedient synthetic strategy to provide diverse 5H-thiazolidin-2,4-diones.

Anti-viral compounds

The present invention relates to compounds of Formula (I) below, which inhibit the growth of picornaviruses, Hepatitus viruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus. wherein: A is phenyl, pyridyl, substituted phenyl, substituted pyridyl, or benzyl; R is hydrogen, COR4, or COCF3; X is N—OH, O, or CHR1; R1is hydrogen, halo, CN, C1-C4alkyl, —C≡CH, CO(C1-C4alkyl), CO2(C1-C4alkyl), or CONR2R3; R2and R3are independently hydrogen or C1-C4alkyl; A′ is hydrogen, halo, C1-C6alkyl, benzyl, naphthyl, thienyl, furyl, pyridyl, pyrollyl, COR4, S(O)nR4, or a group of the formula R4is C1-C6alkyl, phenyl, or substituted phenyl; n is 0, 1, or 2; R5is independently at each occurrence hydrogen or halo; m is 1, 2, 3, or 4; and R6is hydrogen, halo, CF3, OH, CO2H, NH2, NO2, CONHOCH3, C1-C4alkyl, or CO2(C1-C4alkyl), C1-C4alkoxy; or a pharmaceutically acceptable salt thereof.

Quinolinecarboxylic Acids. 3. Synthesis and Antibacterial Evaluation of 2-Substituted-7-oxo-2,3-dihydro-7H-pyridobenzothiazine-6-carboxylic Acids Related to Rufloxacin

A series of 2-substituted-7-oxo-2,3-dihydro-7H-pyridobenzothiazine-6-carboxylic acids has been prepared and evaluated for in vitro antibacterial activity.These derivatives were less active than corresponding desmethylated analogues.Among th