3381-74-6

Upstream product

• 7292-71-9 2-(3-chlorophenyl)glycine 
• 1878-65-5 3-chlorophenylacetic acid 

Downstream Products

• 1105624-44-9 2-(3-chlorophenyl)-2-((3,4-dimethylphenyl)amino)acetic acid 
• 1379946-06-1 3-(5-((3-chlorophenyl)((3,4-dimethylphenyl)amino)methyl)-1,2,4-oxadiazol-3-yl)-N-methylpyridin-2-amine 
• 137420-52-1 (+/-)-α-bromo-(3-chlorophenyl)acetic acid methyl ester 
• 1639055-98-3 2-([1,2,4]triazolo[4',3':1,5][1,2,4]triazolo[4,3-c]thieno-[3,2-e]pyrimidin-9-ylthio)-2-(3-chlorophenyl)acetic acid 
• 1639056-07-7 2-([1,2,4]triazolo[4',3':1,5][1,2,4]triazolo[4,3-c]thieno-[2,3-e]pyrimidin-9-ylthio)-2-(3-chlorophenyl)acetic acid 
• 1092476-47-5 (S)-2-(3-chlorophenyl)-N'-(3,5-dichlorophenyl)-2-(4-methyl-1-piperazinyl)acetohydrazide 
• 1092476-48-6 (R)-2-(3-chlorophenyl)-N'-(3,5-dichlorophenyl)-2-(4-methyl-1-piperazinyl)acetohydrazide 
• 1092477-68-3 (+/-)-2-(3-chlorophenyl)-N'-(3,5-dichlorophenyl)-2-(4-methyl-1-piperazinyl)acetohydrazide 
• 1092477-67-2 (+/-)-(3-chlorophenyl)(4-methyl-1-piperazinyl)acetic acid hydrochloride 

Relevant academic research and scientific papers

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.

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.