Synthesis of a tetronic acid library focused on inhibitors of tyrosine and dual-specificity protein phosphatases and its evaluation regarding VHR and Cdc25B inhibition
Selective inhibitors of protein tyrosine phosphatases (PTPs) and dual-specificity phosphatases (DSPs) are expected to be useful tools for clarifying the biological functions of the PTPs themselves and also to be candidates for novel therapeutics. We planned a library approach for the identification of PTP/DSP inhibitors in which 3-acyltetronic acid is used as a "core" phosphate mimic. A series of novel tetronic acid derivatives were synthesized and evaluated as inhibitors of the dual-specificity protein phosphatases VHR and cdc25B. Several compounds are found to be potent inhibitors of cdc25B, which is a key enzyme for cell-cycle progression. The promising results described herein strongly indicated that this tetronic acid library is potent as a library focused on the PTP/DSP-selective inhibitor.
Sodeoka,Sampe,Kojima,Baba,Usui,Ueda,Osada
p. 3216 - 3222
(2007/10/03)
Alkyl mercaptan process
A process for making alkyl mercaptans in high yield while minimizing the formation of dialkyl sulfides is conducted by reacting an olefin with hydrogen sulfide in an inert solvent (e.g. CH2 Cl2) containing a Lewis Acid catalyst (e.g. BF3). Best results are obtained when the olefin is added to the hydrogen sulfide solution at a rate that keeps the amount of unreacted olefin below about 0.05 moles per mole of hydrogen sulfide.
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(2008/06/13)
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