75257-79-3Relevant articles and documents
Synthesis of an aggregation-induced emission (AIE) active salicylaldehyde based Schiff base: Study of mechanoluminescence and sensitive Zn(II) sensing
Pasha, Sheik Saleem,Yadav, Hare Ram,Choudhury, Angshuman Roy,Laskar, Inamur Rahaman
, p. 9651 - 9658 (2017)
Syntheses of multi-functional Aggregation-Induced Emission (AIE) active molecules in a simple manner have been drawing great attention in current luminescence materials research. In this report a simple diamine molecule (N1-tritylethane-1,2-dia
Comprehensive structure-activity-relationship of azaindoles as highly potent FLT3 inhibitors
Grimm, Sebastian H.,Gagestein, Berend,Keijzer, Jordi F.,Liu, Nora,Wijdeven, Ruud H.,Lenselink, Eelke B.,Tuin, Adriaan W.,van den Nieuwendijk, Adrianus M.C.H.,van Westen, Gerard J.P.,van Boeckel, Constant A.A.,Overkleeft, Herman S.,Neefjes, Jacques,van der Stelt, Mario
supporting information, p. 692 - 699 (2019/01/22)
Acute myeloid leukemia (AML) is characterized by fast progression and low survival rates, in which Fms-like tyrosine kinase 3 (FLT3) receptor mutations have been identified as a driver mutation in cancer progression in a subgroup of AML patients. Clinical trials have shown emergence of drug resistant mutants, emphasizing the ongoing need for new chemical matter to enable the treatment of this disease. Here, we present the discovery and topological structure-activity relationship (SAR) study of analogs of isoquinolinesulfonamide H-89, a well-known PKA inhibitor, as FLT3 inhibitors. Surprisingly, we found that the SAR was not consistent with the observed binding mode of H-89 in PKA. Matched molecular pair analysis resulted in the identification of highly active sub-nanomolar azaindoles as novel FLT3-inhibitors. Structure based modelling using the FLT3 crystal structure suggested an alternative, flipped binding orientation of the new inhibitors.
Efficient Delivery of Quantum Dots into the Cytosol of Cells Using Cell-Penetrating Poly(disulfide)s
Derivery, Emmanuel,Bartolami, Eline,Matile, Stefan,Gonzalez-Gaitan, Marcos
supporting information, p. 10172 - 10175 (2017/08/09)
Quantum dots (QDs) are extremely bright, photostable, nanometer particles broadly used to investigate single molecule dynamics in vitro. However, the use of QDs in vivo to investigate single molecule dynamics is impaired by the absence of an efficient way