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1.
Org Biomol Chem ; 15(14): 2968-2978, 2017 Apr 05.
Artigo em Inglês | MEDLINE | ID: mdl-28294238

RESUMO

The acid-promoted crystallization-induced diastereoisomer transformation (CIDT) of naphthoxazines derived from racemic O-protected 2-substituted 4-hydroxybutyraldehydes and enantiopure Betti's base allows the deracemization of the starting aldehydes with ee up to 96%. As an alternative, reduction with lithium aluminum hydride of the diastereoisomerically enriched naphthoxazines leads to enantioenriched primary amines. The utility of the latter strategy was demonstrated by applying it to the synthesis of enantioenriched fenpropimorph and to the first synthesis of enantiopure amorolfine, with ee up to 99.5%.


Assuntos
Aldeídos/química , Morfolinas/química , Morfolinas/síntese química , Técnicas de Química Sintética , Cristalização , Modelos Moleculares , Conformação Molecular , Estereoisomerismo
2.
Curr Cancer Drug Targets ; 13(7): 749-54, 2013 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23952099

RESUMO

Tyrosin kinase inhibitors (TKI), have dramatically changed the natural history of chronic myeloid leukemia (CML) leading to an impressive increase in overall survival rates and allowing many CML patients to achieve a close-to-normal life expectancy. Unfortunately, there is growing evidence that these drugs are not curative, about 30-35% of the patients who receive imatinib become resistant or discontinue the drug because of side effects; moreover, 15% of all patients become resistant to all TKIs, a condition which represents the biggest challenge in CML treatment. Recent progresses in CML stem cell biology have identified new agents and therapeutic strategies that can be used to target the CML stem cell compartment. These studies have opened new perspectives and have highlighted key strategies for treating, and possibly curing, CML in the upcoming years.


Assuntos
Antineoplásicos/uso terapêutico , Leucemia Mielogênica Crônica BCR-ABL Positiva/tratamento farmacológico , Células-Tronco Neoplásicas/efeitos dos fármacos , Inibidores de Proteínas Quinases/uso terapêutico , Proteínas Tirosina Quinases/antagonistas & inibidores , Animais , Antineoplásicos/efeitos adversos , Antineoplásicos/química , Desenho de Fármacos , Resistencia a Medicamentos Antineoplásicos , Humanos , Leucemia Mielogênica Crônica BCR-ABL Positiva/enzimologia , Leucemia Mielogênica Crônica BCR-ABL Positiva/patologia , Terapia de Alvo Molecular , Estadiamento de Neoplasias , Células-Tronco Neoplásicas/metabolismo , Células-Tronco Neoplásicas/patologia , Inibidores de Proteínas Quinases/efeitos adversos , Inibidores de Proteínas Quinases/química , Proteínas Tirosina Quinases/metabolismo , Transdução de Sinais/efeitos dos fármacos
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