149267-74-3Relevant academic research and scientific papers
Synthesis and Superpotent Anticancer Activity of Tubulysins Carrying Non-hydrolysable N-Substituents on Tubuvaline
Sani, Monica,Lazzari, Paolo,Folini, Marco,Spiga, Marco,Zuco, Valentina,De Cesare, Michelandrea,Manca, Ilaria,Dall'Angelo, Sergio,Frigerio, Massimo,Usai, Igor,Testa, Andrea,Zaffaroni, Nadia,Zanda, Matteo
, p. 5842 - 5850 (2017)
Synthetic tubulysins 24 a–m, containing non-hydrolysable N-substituents on tubuvaline (Tuv), were obtained in high purity and good overall yields using a multistep synthesis. A key step was the formation of differently N-substituted Ile-Tuv fragments 10 b
Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith
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Page/Page column 49, (2008/12/07)
Provided herein are Heterocyclic Compounds having the following structure: wherein R1, R2, X, Y and Z are as defined herein, compositions comprising an effective amount of a Heterocyclic Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heterocyclic Compound to a patient in need thereof.
BENZO[C][2,7]NAPHTHYRIDINE DERIVATIVES, AND THEIR USE AS KINASE INHIBITORS
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Page/Page column 194, (2008/12/08)
The present invention relates to Benzo[c] [2,7] naph thy ri dine Derivatives of formula (I), compositions comprising an effective amount of a Benzo[c] [2,7]naphthyridine Derivative, methods for treating or preventing a proliferative disorder or an autoimmune disease, comprising administering to a subject in need thereof an effective amount of a Benzo[c] [2,7]naphthyridine Derivative, methods for modulating PDK-I activity, PKA activity, Akt activity, S6K activity, or PKC activity, comprising administering to a subject in need thereof an effective amount of a Benzo[c] [2,7] naphthyridine Derivative. The invention also relates to processes for preparing a Benzo[c] [2,7] naphthyridine Derivative.
Antiretroviral hydrazine derivatives
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, (2008/06/13)
The invention relates to compounds of formula STR1 and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.
SYNTHESIS AND BIOLOGICAL ACTIVITIES OF BRADYKININ ANALOGUES WITH Ψ(E,CH=CH) AND Ψ(CH2-NH) ISOSTERIC PEPTIDE BOND REPLACEMENTS
Scarso, A.,Degelaen, J.,Viville, R.,Cock, E. De,Marsenille, M. Van,et al.
, p. 381 - 399 (2007/10/02)
The synthesis of bradykinin analogues is described in which the Gly4-Phe5, Phe5-Ser6 or the Pro7-Phe8 peptide bond has been replaced by a trans carbon-carbon double bond or by a "reduced" peptide bond.Some of the analogues display high potency and prolonged activity in the rat blood pressure test, indicating increased metabolic stability.A clear selectivity is obtained towards the myotropic effect in the guinea pig ileum.
