- COVALENT RAS INHIBITORS AND USES THEREOF
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The disclosure features compounds, or pharmaceutically acceptable salts thereof, alone and in combination with other therapeutic agents, pharmaceutical compositions, and protein conjugates thereof, capable of modulating biological processes including Ras, and their uses in the treatment of cancers.
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- RAS INHIBITORS
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The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.
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- Selective cleavage of carbamate protecting groups from aziridines with otera's catalyst
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Otera's distannoxane catalyst was found to promote the cleavage of carbamate groups from N-protected aziridines. This method enables the chemoselective cleavage of an aziridinyl N-carbobenzyloxy (Cbz) group in the presence of other N-Cbz groups. The selec
- Sun, Shan,Tirotta, Ilaria,Zia, Nicholas,Hutton, Craig A.
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p. 411 - 415
(2014/04/03)
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- On The Synthesis of (2S)-Aziridine-2-Carboxylic Acid Containing Peptides
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Optimized conditions are described for the synthesis of 1-trityl-2-aziridine-carboxylic acid 3 (Trt-Azy-OH) and benzyl (2S)-aziridine-2-carboxylate 6 (H-Azy-OBzl) as useful derivatives for the synthesis of N- and C-terminal aziridine-containing peptides.Thereby, the use of the pentafluorophenyl ester of Trt-Azy-OH was found to be the method of choice in acylating steps, whereas acylation of H-Azy-OBzl several classical methods of peptide synthesis can be succesfully used.The fully protected aziridine-2-carboxylic acid peptides are accessible in satisfactory yields as analytically defined products, but partial or total deprotection of these compounds again by standard procedures of peptide synthesis is surprisingly difficult in terms of satisfactory yields, whereby sequence-dependent unstability both in the reaction and purification steps as well as on storage was found to strongly limit the accessibility of these aziridine-containing peptides as promising active-site inactivators of cysteine-proteinases.
- Korn, Andreas,Rudolph-Boehner, Sabine,Moroder, Luis
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p. 1717 - 1730
(2007/10/02)
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- An expeditious in situ preparation of benzyl (S)-2-aziridinecarboxylate
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The use of diethoxytriphenylphosphorane in the preparation of benzyl (S)-2-aziridinecarboxylate is illustrated.The latter compound has been coupled with Z-Ala-OH and the aziridine dipeptide thus obtained ring-opened via C-3-N-1 cleavage with benzyl alcoho
- Kuyl-Yeheskiely, E.,Dreef-Tromp, C. M.,Marel, G. A. van der,Boom, J. H. van
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p. 314 - 316
(2007/10/02)
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- PREPARATION AND PROPERTIES OF S,S-DIPHENYL AMINO ACID PHOSPHORODITHIOATES
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S,S-diphenyl phosphorodithioates of appropriately protected serine and tyrosine have been prepared.In the case of serine, neighbouring group participation of a free N- or C-terminus on the corresponding triester functions leads to the formation of aziridi
- Kuyl-Yeheskiely, E.,Tromp, C. M.,Geluk, A.,Marel, G. A. van der,Boom, J. H. van
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p. 566 - 569
(2007/10/02)
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