RESUMO
Retinoids are analogues of all-trans-retinoic acid, a powerful hormone that mediates many fundamental biological processes. Cancer and other serious hyperproliferative diseases are attractive therapeutic targets for retinoids, but the therapeutic use of retinoids is limited due to severe toxicity. We report here the design of retinoid receptor-alpha specific ligands with growth inhibitory activity in breast cancer cell lines, and which do not cause the cutaneous toxicity associated with the currently available nonselective retinoid agonists.
Assuntos
Amidas/síntese química , Amidas/farmacologia , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Receptores do Ácido Retinoico/efeitos dos fármacos , Amidas/toxicidade , Antineoplásicos/toxicidade , Neoplasias da Mama/tratamento farmacológico , Feminino , Humanos , Ligação de Hidrogênio , Receptor alfa de Ácido Retinoico , Retinoides/síntese química , Retinoides/farmacologia , Retinoides/toxicidade , Relação Estrutura-AtividadeRESUMO
Catalytic hydrogenation of various azides in the presence of functionalized mixed carbonates afforded the corresponding urethanes in high yields.
RESUMO
An efficient and mild method for alkoxycarbonylation of amines is described, utilizing commercially available N,N'-disuccinimidyl carbonate.
RESUMO
Boron enolates obtained from optically active oxazolidinone derivative of cis-1-amino-2-hydroxyindan are reacted with various aldehydes to provide highly enantioselective aldol products in good yields.
RESUMO
The reaction of di(2-pyridyl) carbonate with a variety of alcohols including hindered secondary, tertiary and protected glycols afforded the corresponding mixed carbonate which was efficiently transformed into various carbamates in high yield under mild conditions.