1616795-50-6Relevant articles and documents
Deaminative Arylation of Amino Acid-derived Pyridinium Salts
Hoerrner, Megan E.,Baker, Kristen M.,Basch, Corey H.,Bampo, Earl M.,Watson, Mary P.
supporting information, p. 7356 - 7360 (2019/09/30)
A Suzuki-Miyaura cross-coupling of α-pyridinium esters and arylboroxines has been developed. Combined with formation of the pyridinium salts from amino acid derivatives, this method enables amino acid derivatives to be efficiently transformed into α-aryl
RE12 derivatives displaying Vaccinia H1-related phosphatase (VHR) inhibition in the presence of detergent and their anti-proliferative activity against HeLa cells
Thuaud, Frederic,Kojima, Shuntaro,Hirai, Go,Oonuma, Kana,Tsuchiya, Ayako,Uchida, Takako,Tsuchimoto, Teruhisa,Sodeoka, Mikiko
, p. 2771 - 2782 (2014/05/06)
New derivatives of Vaccinia H1-related phosphatase (VHR) inhibitor RE12 (5) were designed by replacing the long straight alkyl chain with other hydrophobic functionalities containing two aromatic rings, with the aim of obtaining potent, cell-active inhibitors. We established a direct coupling reaction between tetronic acid derivative and thioimidate to prepare the RE derivatives 6a-6i efficiently. These compounds all showed VHR-inhibitory activity in the presence of 0.001% NP-40, whereas RE12 (5) was inactive under this condition, even at 100 μM. Further structure-activity studies focused on terminal substitution afforded trifluoromethyl derivative 6k (RE176) and nitro derivative 6l (RE177). The IC50 value of 6l in the presence of NP-40 was almost equivalent to that of RE12 (5) in its absence. Compound 6k (RE176) potently inhibited proliferation of HeLa cells.
