197079-39-3Relevant articles and documents
Practical Gram-Scale Synthesis of Iboxamycin, a Potent Antibiotic Candidate
Mason, Jeremy D.,Myers, Andrew G.,Pote, Aditya R.,Terwilliger, Daniel W.
, p. 11019 - 11025 (2021/08/03)
A gram-scale synthesis of iboxamycin, an antibiotic candidate bearing a fused bicyclic amino acid residue, is presented. A pivotal transformation in the route involves an intramolecular hydrosilylation-oxidation sequence to set the ring-fusion stereocenters of the bicyclic scaffold. Other notable features of the synthesis include a high-yielding, highly diastereoselective alkylation of a pseudoephenamine amide, a convergent sp3-sp2 Negishi coupling, and a one-pot transacetalization-reduction reaction to form the target compound's oxepane ring. Implementation of this synthetic strategy has provided ample quantities of iboxamycin to allow for its in vivo profiling in murine models of infection.
Structure-activity relationships of monomeric C2-aryl pyrrolo[2,1- c ][1,4]benzodiazepine (PBD) antitumor agents
Antonow, Dyeison,Kaliszczak, MacIej,Kang, Gyoung-Dong,Coffils, Marissa,Tiberghien, Arnaud C.,Cooper, Nectaroula,Barata, Teresa,Heidelberger, Sibylle,James, Colin H.,Zloh, Mire,Jenkins, Terence C.,Reszka, Anthony P.,Neidle, Stephen,Guichard, Sylvie M.,Jodrell, Duncan I.,Hartley, John A.,Howard, Philip W.,Thurston, David E.
experimental part, p. 2927 - 2941 (2010/09/14)
A comprehensive SAR investigation of the C2-position of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) monomer antitumor agents is reported, establishing the molecular requirements for optimal in vitro cytotoxicity and DNA-binding affinity. Both carbocyclic and
Spirocycle integrin inhibitors
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, (2008/06/13)
This invention relates to novel heterocycles, including (S)-2-phenylsulfonylamino-3-???8-(2-pyridinylaminomethyl)-!-1-oxa-2-azaspiro-?4,5!-dec-2-en-3-yl!carbonylamino! propionic acid, which are useful as antagonists of the αv β3 inte