7357-66-6Relevant academic research and scientific papers
METHODS AND COMPOSITIONS FOR MODULATING SPLICING
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Paragraph 0620; 0712, (2020/08/22)
Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions.
Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors
Hasvold, Lisa A.,Wang, Le,Przytulinska, Magdalena,Xiao, Zhan,Chen, Zehan,Gu, Wen-Zhen,Merta, Philip J.,Xue, John,Kovar, Peter,Zhang, Haiying,Park, Chang,Sowin, Thomas J.,Rosenberg, Saul H.,Lin, Nan-Horng
, p. 2311 - 2315 (2008/09/21)
The synthesis and structure-activity relationships (SAR) of Chk1 inhibitors based on a 5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-one core are described. Specifically, an exploration of the 7 and 8 positions on this previously disclosed core afforded compounds with improved enzymatic and cellular potency.
Synthesis and anti-breast cancer activities of substituted quinolines
Shi, Aibin,Nguyen, Thu A.,Battina, Srinivas K.,Rana, Sandeep,Takemoto, Dolores J.,Chiang, Peter K.,Hua, Duy H.
body text, p. 3364 - 3368 (2009/04/11)
Promising anti-breast cancer agents derived from substituted quinolines were discovered. The quinolines were readily synthesized in a large scale from a sequence of reactions starting from 4-acetamidoanisole. The Michael addition product was isolated as the reaction intermediate in the ring closing reaction of 4-amino-5-nitro-2-(3-trifluoromethylphenyloxy)anisole with methyl vinyl ketone leading to 6-methoxy-4-methyl-8-nitro-5-(3-trifluoromethylphenyloxy)quinoline (14). The amino function of 8-amino-6-methoxy-4-methyl-5-(3-trifluoromethylphenyloxy)quinoline, prepared from 14, was connected to various side chains via alkylation with N-(3-iodopropyl)phthalimide, Michael addition with acrylonitrile, and reductive amination with various heterocycle carboxaldehydes, such as imidazole-4-carboxaldehyde, thiophene-2-carboxaldehyde, and 2-furaldehyde. Effects of the substituted quinolines on cell viability of T47D breast cancer cells using trypan blue exclusion assay were examined. The results showed that the IC50 value of 6-methoxy-8-[(2-furanylmethyl)amino]-4-methyl-5-(3-trifluoromethylphenyl oxy)quinoline is 16 ± 3 nM, the lowest IC50 out of all the quinolines tested. IC50 values of three other quinolines are in the nanomolar range, a desirable range for pharmacological testing.
COMPOUNDS AFFECTING GAP JUNCTION ACTIVITY
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Page/Page column 12-13; 17, (2008/06/13)
ThThis invention relates to novel quinoline compounds which affect gap junction activity. Also provided are methods of using such compounds and compositions containing the compounds to treat gap junction disorders.
HETEROCYCLIC KINASE INHIBITORS
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Page 144, (2010/02/08)
Compounds having the formula (I) are useful for inhibiting protein kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
Heterocyclic Systems Containing Bridgehead Nitrogen Atom: Part LIV - Synthesis of Thiazolobenzimidazol-3-(2H)-ones
Bindal, Varinder,Jain, Kiran,Handa, R. N.,Pujari, H. K.
, p. 807 - 811 (2007/10/02)
3-Bromo-4-methoxyacetanilide (V) on nitration with fuming nitric acid in the presence of acetic anhydride gives 3-bromo-4-methoxy-6-nitroacetanilide (VI) which on hydrolysis and subsequent reduction of the nitroaniline (IX) followed by the treatment of th
