RESUMO
Treatment of oxazolidinediones with TiCl4 in CH2Cl2 resulted in conversion to isoindoloisoquinolinones via intramolecular FriedelCrafts reaction with extrusion of CO2 in the transformation. The alkaloid nuevamine has been synthesized under these conditions in a regiospecific manner.
RESUMO
A series of amide and urea derivatives of benzothiazole have been synthesized and evaluated for their antiproliferative profile in human SK-Hep-1 (liver), MDA-MB-231 (breast), and NUGC-3 (gastric) cell lines. Among them, compounds 1-2, 16-18, 23, and 25-26 had potent to moderate inhibitory activities. Further these compounds were investigated for their ability to inhibit Raf-1 activity.
Assuntos
Amidas/síntese química , Benzotiazóis/farmacologia , Inibidores de Proteínas Quinases/farmacologia , Proteínas Proto-Oncogênicas c-raf/antagonistas & inibidores , Ureia/síntese química , Benzotiazóis/síntese química , Benzotiazóis/química , Linhagem Celular Tumoral , Humanos , Espectroscopia de Ressonância Magnética , Inibidores de Proteínas Quinases/síntese química , Inibidores de Proteínas Quinases/química , Espectrometria de Massas por Ionização por ElectrosprayRESUMO
Several nucleophiles such as proteins or poly(ethyleneimine) could be easily conjugated with a 11-(2,4-dinitro-5-fluorobenzene)undecenamide (DFUA) monolayer photochemically prepared on a silicon (100) surface.
Assuntos
Alcanos/química , Amidas/química , Fluorbenzenos/química , Hidrogênio/química , Proteínas/química , Silício/química , Íons/química , Estrutura Molecular , Fotoquímica , Propriedades de Superfície , Água/químicaRESUMO
Palladium-catalyzed arylation of alpha,beta-unsaturated gamma-lactam, which could be prepared by condensation of amines and keto-esters, has been carried out to make the core structure of Erythrina alkaloids.
Assuntos
Alcaloides/síntese química , Erythrina/química , Lactamas/química , Paládio/química , Aminas/química , Catálise , Ciclização , Ésteres , Cetonas/química , Conformação MolecularRESUMO
(+)-Monomorine has been synthesized under mild hydrogenation conditions initiating deprotection followed by intramolecular, sequential reductive amination reactions. The precursors could be prepared concisely using B-alkyl Suzuki cross coupling of a chiral homoallylamine and a vinyl iodide or an iodofuran derivative.
Assuntos
Alcaloides/síntese química , Técnicas de Química Combinatória , Indolizinas/síntese química , Catálise , Hidrogenação , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , EstereoisomerismoRESUMO
A series of 4-(N-imidazol-2-ylmethyl)aminobenzopyran analogues, originally designed as K(ATP) openers for ischemic diseases, showed antiangiogenic properties through the inhibition of HUVEC tube formation. Especially one of p-Cl substituted analogues (4c) completely inhibited HUVEC tube formation at 10 microM. The compound 4c significantly inhibited tumor growth by 52% on A549 (human non small cell lung carcinoma) in nude mice xenografts without any significant side effects.
Assuntos
Inibidores da Angiogênese/síntese química , Inibidores da Angiogênese/farmacologia , Inibidores da Angiogênese/toxicidade , Animais , Antineoplásicos/síntese química , Antineoplásicos/farmacologia , Antineoplásicos/toxicidade , Linhagem Celular Tumoral , Células Endoteliais/efeitos dos fármacos , Humanos , Camundongos , Camundongos Nus , Neoplasias Experimentais/complicações , Neoplasias Experimentais/tratamento farmacológico , Relação Estrutura-Atividade , Transplante Heterólogo , Resultado do Tratamento , Veias Umbilicais/citologiaRESUMO
Calixcrown-6 compounds carrying a pair of phenylazo moieties on the upper rim and two OH groups, one OH group, and two OR groups on the lower rim have been prepared in both the cone and partial cone conformations. UV/vis spectral measurements showed a red shift upon the addition of Ca2+ to the calixcrown carrying two OH groups and a blue shift for the calixcrown carrying two OR groups. For the compounds with two OR groups on the lower rim and a fixed partial cone conformation, a blue shift caused by electrostatic interaction between the oxygen atoms of OR and the metal ion as well as a red shift caused by the pi-metal complexation between the rotated calix benzene and the metal ion were observed.