1351815-34-3Relevant academic research and scientific papers
Extended Piperidine-Piperidinone Protein Interface Mimics
Xin, Dongyue,Raghuraman, Arjun,Burgess, Kevin
, p. 4450 - 4458 (2015)
Minimalist structures, H and I, were designed as protein interface mimics. Attributes of these chemotypes are (i) greater rigidity than conventional peptides, (ii) chiral and nonplanar heterocyclic backbones that are less prone to the hydrophobic aggregation effects, and (iii) potential to be prepared with a variety of side chains corresponding to natural amino acids. Intermediates, however, in the oligo(pyrrolidinone-piperidine)s H syntheses were vulnerable to epimerization. The origins of this epimerization were determined, then the study was focused on oligo(piperidinone-piperidine) compounds I. Mimics I were prepared via iterative couplings; a penta(piperidinone-piperidine) was prepared in this way. A series of lower homologues of this pentamer were crystallized and studied (single crystal X-ray), and four of them were used in a circular dichroism (CD) study. Thus, an estimate of 36 ? for the N-to-C distance of a typical conformation of the penta(piperidinone-piperidine) was made. CD spectra of four progressively longer oligomers allowed assignment of elipticity changes around 300 nm that can be attributed to increased conformational ordering of the longer oligomers in solution. (Chemical Equation Presented).
BENZAMIDE DERIVATIVES AND THEIR USE AS HSP90 INHIBTORS
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Page/Page column 57-58, (2012/01/05)
The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
