52797-54-3Relevant articles and documents
Minimum structural requirements for inhibitors of the zinc finger protein TRAF6
Radwan, Mohamed O.,Koga,Hida, Tomohiro,Ejima, Tomohiko,Kanemaru, Yosuke,Tateishi, Hiroshi,Okamoto, Yoshinari,Inoue, Jun-ichiro,Fujita, Mikako,Otsuka, Masami
, p. 2162 - 2167 (2019)
Zinc fingers have rarely been regarded as drug targets. On the contrary, the zinc-binding site of enzymes has often been considered a target of inhibitors. We previously developed a dithiol compound called SN-1 that binds to the zinc finger protein tumor necrosis factor receptor-associated factor 6 (TRAF6) and suppresses downstream nuclear factor-κB (NF-κB) signaling. To determine the minimal structure requirements of TRAF6 inhibitors based on SN-1, NF-κB inhibitory activity and cytotoxicity of its derivatives including new compounds were examined. SN-2, an oxidative type of prodrug of SN-1 with 2-nitrophenylthio groups via disulfide, has the minimum structure for an inhibitor of TRAF6, as seen with cellular experiments. The importance of two side chains with a thiol group was shown with molecular modelling. This study may lead to development of selective TRAF6 inhibitors in the near future.
Synthesis and structural characterisation of neutral pentacoordinate silicon(iv) complexes with a tridentate dianionic N,N,S chelate ligand
Kobelt, Claudia,Burschka, Christian,Bertermann, Ruediger,Fonseca Guerra,Bickelhaupt, F. Matthias,Tacke, Reinhold
experimental part, p. 2148 - 2162 (2012/03/22)
A series of novel neutral pentacoordinate silicon(iv) complexes with SiClSN2C, SiBrSN2C, SiSN3C, SiSON2C, SiS2N2C, SiSeSN2C and SiTeSN2C skeletons (compounds 1-12) was
Zinc complexes of the N,N,S ligand (mercaptophenyl)(picolyl)amine
Brand, Udo,Vahrenkamp, Heinrich
, p. 435 - 440 (2007/10/03)
The zinc complex chemistry of the tridentate thiol ligand N-(2-mercaptophenyl)(2-picolyl)amine (MPPAH) differs considerably from that of the aliphatic analogue N-(2-mercaptoethyl)(2-picolyl)amine reported previously. This is due to the lower basicity and hence bridging tendency of its aromatic thiolate function. With zinc salts of oxo anions the 1:1 complexes (MPPA)ZnX (1a-c: X = ONO2, OAc, OBz) are formed which according to spectroscopic data are monomeric while the halide (MPPA)ZnBr (2) seems to be polymeric. In the absence of coordinating anions the monomeric 2:1 complex (MPPA)2Zn (3) results which according to a crystal structure determination contains tetrahedral zinc coordinated by one MPPA ligand in a tridentate fashion while the other is only monodentate and sulfur-bound. A similar N2S2 coordination can be deduced for the 1:1:1 complex (MPPA)Zn(STrt) (4) resulting from ZnEt2, MPPAH and triphenylmethanethiol. VCH Verlagigesdlschaft mbH, 1996.