16634-91-6Relevant academic research and scientific papers
NEW FYN AND VEGFR2 KINASE INHIBITORS
-
Page/Page column 25, (2021/06/22)
The invention relates to a N-phenylcarbamoyl compound of Formula (I) or a pharmaceutically acceptable salt thereof for use in the inhibition of at least one of tyrosine kinase selected from Fyn and VEGFR2 in the treatment of diseases and disorders involved with one or both kinases. (Formula)
BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS AND USES THEREOF
-
, (2017/02/28)
β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS
-
, (2015/09/22)
β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
BETA-SUBSTITUTED GAMMA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS
-
, (2015/09/22)
β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.
A simple and convenient manganese dioxide oxidation of benzyl halides to aromatic aldehydes under neutral condition
Goswami, Shyamaprosad,Jana, Subrata,Dey, Swapan,Adak, Avijit Kumar
, p. 194 - 195 (2007/10/03)
A simple, convenient and inexpensive benzylic oxidation reaction of arylmethylhalides under neutral conditions by manganese dioxide to the corresponding aldehydes has been described. Copyright
4-Imidazole derivatives of benzyl and restricted benzyl sulfonamides, sulfamides, ureas, carbamates, and amides and their use
-
, (2008/06/13)
Compounds of formula I are useful in treating diseases prevented by or ameliorated with α1A agonists. Also disclosed are α1A agonist compositions and a method of activating α1 adrenoceptors in a mammal.
Nitroarylhydroxymethylphosphonic acids as inhibitors of CD45
Beers, Scott A.,Malloy, Elizabeth A.,Wu, Wei,Wachter, Michael P.,Gunnia, Uma,Cavender, Druie,Harris, Crafford,Davis, Janet,Brosius, Ruth,Pellegrino-Gensey, J. Lee,Siekierka, John
, p. 2203 - 2211 (2007/10/03)
A series of nitroarylhydroxymethylphosphonic acids was synthesized and evaluated as inhibitors of CD45. It was discovered that both the alpha hydroxy and nitro groups are essential for activity. Potency is enhanced by the addition of a large lipophilic group on the aryl ring adjacent to the phosphonic acid moiety. Kinetics studies have shown that these compounds are competitive inhibitors and thus bind at the active site of this enzyme.
Potential antisecretory antidiarrheals. 1. α2-Adrenergic aromatic aminoguanidine hydrazones
Pitzele,Moormann,Gullikson,Albin,Bianchi,Palicharla,Sanguinetti,Walters
, p. 138 - 144 (2007/10/02)
Guanabenz, a centrally acting antihypertensive agent, has been shown to have intestinal antisecretory properties. A series of aromatic aminoguanidine hydrazones was made in an effort to separate the antisecretory and cardiovascular activities. Benzaldehyde, naphthaldehyde, and tetralone derivatives were synthesized. The compounds were evaluated in the cholera toxin treated ligated jejunum of the rat and in the Ussing chamber using a rabbit ileum preparation. A number of compounds, including members of each structural class, were active upon subcutaneous administration in the rat. Active compounds were determined to be α2-adrenergic agonists by yohimbine reversals of their Ussing chamber activities. The compound displaying the best separation of activities was the aminoguanidine hydrazone of 2,6-dimethyl-4-hydroxybenzaldehyde (20).
Comparative Reactivity of Substituted 4-Nitrobenzylidene Dichlorides with Alkali
Goh, Swee Hock,Kam, Toh Seok
, p. 423 - 426 (2007/10/02)
A comparative study of the reactions of substituted 4-nitrobenzylidene dichlorides ArCHCl2 (Ar = 3-Cl-4-NO2C6H3, 2-Cl-4-NO2C6H3, 4-NO2C6H4, 3,5-Me2-4-NO2C6H2, and 2-Me-4-NO2C6H3) with aqueous alcoholic alkali shows that chlorine substitution enhances the
