منابع مشابه
Artificial Macrocycles as Potent p53–MDM2 Inhibitors
Based on a combination of an Ugi four component reaction and a ring closing metathesis, a library of novel artificial macrocyclic inhibitors of the p53-MDM2 interaction was designed and synthesized. These macrocycles, alternatively to stapled peptides, target for the first time the large hydrophobic surface area formed by Tyr67, Gln72, His73, Val93, and Lys94 yielding derivatives with affinity ...
متن کاملMacrocycles and constrained peptides
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متن کاملTwo oxazane macrocycles.
The 20-membered ring in 1,7,11,17-tetraoxa-2,6,12,16-tetraazacycloeicosane tetrahydrochloride, C(12)H(32)N(4)O(4)(4+).4Cl(-), adopts an endo conformation, while the 18-membered ring in 1,6,10,15-tetraoxa-2,5,11,14-tetraazacyclooctadecane tetrahydrochloride, C(10)H(28)N(4)O(4)(4+).4Cl(-), lies about an inversion centre and adopts a symmetrical conformation. In the crystal structures of both comp...
متن کاملHow Proteins Bind Macrocycles
The potential utility of synthetic macrocycles (MCs) as drugs, particularly against low-druggability targets such as protein-protein interactions, has been widely discussed. There is little information, however, to guide the design of MCs for good target protein-binding activity or bioavailability. To address this knowledge gap, we analyze the binding modes of a representative set of MC-protein...
متن کاملNon-aggregational aromatic oligoamide macrocycles.
Attaching peripheral amide groups to the backbone of cyclic aromatic oligoamides 1 leads to new macrocycles 2 that show drastically changed behavior including modest yields of formation and no tendency to aggregate while maintaining a rigid backbone and a defined, guest-binding internal cavity.
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ژورنال
عنوان ژورنال: Synlett
سال: 2018
ISSN: 0936-5214,1437-2096
DOI: 10.1055/s-0036-1591975