938083-50-2Relevant academic research and scientific papers
Synthesis of bisboron compounds and their strong inhibitory activity on store-operated calcium entry
Suzuki, Akinobu Z.,Ozaki, Shoichiro,Goto, Jun-Ichi,Mikoshiba, Katsuhiko
experimental part, p. 1395 - 1398 (2010/06/19)
Store-operated calcium entry (SOCE) is an important mechanism for replenishing intracellular calcium stores and for sustaining calcium signaling. We developed a method for synthesis of bisboron compounds that have two borinic acids or their esters in one molecule. These compounds are analogues of 2-APB, which is widely used as a membrane-permeable SOCE inhibitor. Further, we examined the effect of the newly synthesized bisboron compounds on SOCE in Jurkat T cells. All the bisboron compounds showed strong inhibitory activity on SOCE, with IC50 values of less than 1 μM, which were 20-45 times lower than observed with 2-APB.
NOVEL BISBORON COMPOUND
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Page/Page column 20, (2008/12/08)
A bisboron compound represented by the general formula (I): wherein B represents a boron atom, Y represents an oxygen or sulfur atom, R1 and R2 independently represent a monocyclic aromatic group, a polycyclic aromatic group, or a heterocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur atoms, R3 represents a hydrogen atom; -(CH2)m-NR4R5; -CO-(CH2)m-NR4R5; - COCH(NH2)R6; -CHR7R8; -CH2CH(NH2)-R9; quinolyl substituted with C1-C4 alkyl group; or C1-C4 alkyl substituted with pyridyl, piperidino or pyrrolidinyl group, and X represents a monocyclic atomatic group, a polycyclic aromatic group or a heterocyclic group, which may be the same as or different from R1 and R2, or a bifunctional group having a monocyclic aromatic group, polycyclic aromatic group or heterocyclic group bonded to each side of a group selected from the group consisting of a single bond, O, CH2, S, SO2, CH2OCH2, OCH2, OCH2CH2OCH2, OCH2OCH2CH2 and CH2OCH2CH2, or a salt thereof, and a composition for controlling the intracellular calcium concentration, which comprises the compound or salt thereof as an active ingredient.
