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1.
Org Biomol Chem ; 21(44): 8813-8818, 2023 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-37889185

RESUMEN

In four simple steps, a series of 5H-thiazolo[2',3':2,3]imidazo[4,5-b]indole and 11H-benzo[4',5']thiazolo[2',3':2,3]imidazo[4,5-b]indole derivatives were prepared with high yields. The key step in this procedure was demonstrated to be two-fold Cu-catalysed C-N coupling reactions of 5-bromo-6-(2-bromophenyl)imidazo[2,1-b]thiazole and 3-bromo-2-(2-bromophenyl)benzo[d]imidazo[2,1-b]thiazole with various amines.

2.
RSC Adv ; 14(40): 29535-29541, 2024 Sep 12.
Artículo en Inglés | MEDLINE | ID: mdl-39297035

RESUMEN

In a new approach, a series of 3-aroylimidazo[1,2-a]pyridine derivatives were prepared in high yields. This approach revealed the direct Fe-catalyzed functionalization of imidazo[1,2-a]pyridine derivatives with aryl aldehydes via an aerobic oxidative cross-dehydrogenative coupling process. This transformation occurred in the presence of air, and FeBr3 served as a homogeneous Lewis catalyst. O2 was found to be the principal oxidant responsible for the method's success. Interestingly, when these reactions were carried out under an argon atmosphere, 3,3'-(arylmethylene)bis(2-phenylimidazo[1,2-a]pyridines) derivatives were prepared in good yields.

3.
ChemMedChem ; 19(18): e202400316, 2024 Sep 16.
Artículo en Inglés | MEDLINE | ID: mdl-38856518

RESUMEN

We are reporting a short and convenient pathway for the synthesis of novel ß-carboline-bisindole hybrid compounds from relatively cheap and commercially available chemicals such as tryptamine, dialdehydes and indoles. These newly designed compounds can also be prepared in high yields with the tolerance of many functional groups under mild conditions. Notably, these ß-carboline-bisindole hybrid compounds exhibited some promising applications as anticancer agents against the three common cancer cell lines MCF-7 (breast cancer), SK-LU-1 (lung cancer), and HepG2 (liver cancer). The two best compounds 5 b and 5 g inhibited the aforementioned cell lines with the same IC50 range of the reference Ellipticine at less than 2 µM. A molecular docking study to gain more information about the interactions between the synthesized molecules and the kinase domain of the EGFR was performed. Therefore, this finding can have significant impacts on the development of future research in medicinal chemistry and drug discovery.


Asunto(s)
Antineoplásicos , Carbolinas , Diseño de Fármacos , Ensayos de Selección de Medicamentos Antitumorales , Indoles , Simulación del Acoplamiento Molecular , Humanos , Carbolinas/química , Carbolinas/farmacología , Carbolinas/síntesis química , Antineoplásicos/farmacología , Antineoplásicos/síntesis química , Antineoplásicos/química , Indoles/química , Indoles/farmacología , Indoles/síntesis química , Relación Estructura-Actividad , Línea Celular Tumoral , Receptores ErbB/antagonistas & inhibidores , Receptores ErbB/metabolismo , Proliferación Celular/efectos de los fármacos , Estructura Molecular , Relación Dosis-Respuesta a Droga , Sitios de Unión , Células Hep G2
4.
Chem Commun (Camb) ; 59(14): 1947-1950, 2023 Feb 14.
Artículo en Inglés | MEDLINE | ID: mdl-36637415

RESUMEN

A practical strategy for the iodine-promoted synthesis of bis(1-imidazo[1,5-a]pyridyl)arylmethane and its derivatives has been developed. These compounds exhibit high cytotoxicity toward various cancer cell lines and moreover they are promising ligands for the Cu-catalysed synthesis of quinolines.

5.
Curr Org Synth ; 20(8): 880-889, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-36856172

RESUMEN

AIMS: Synthesis of 1,4-Dihydropyridines (1,4-DHP) using heterogeneous catalyst under mild condition. OBJECTIVE: Our objective is to explore new applications of non-metal heterogeneous catalysts in the synthesis of 1,4-DHP derivatives in a greener and more efficient approach. METHODS: A greener and more efficient method for the synthesis of 1,4-DHPs and an asymmetric 1,4-DHP (Felodipine drug) was successfully developed in high yields using a heterogeneous SBA- 15-SO3H catalyst. RESULTS: A series of symmetric 1,4-DHP and an asymmetric 1,4-DHP (Felodipine drug) were successfully prepared in high yields using a heterogeneous SBA-15-SO3H catalyst. CONCLUSION: The catalyst, SBA-15-SO3H, exhibited an efficient catalyst activity for the synthesis of 1,4-DHP derivatives in high yields from the aldehyde, ß-ketoester, and NH4OAc as a nitrogen source under mild conditions and short reaction time. Bronsted acid sites of this solid catalyst were figured out to play a key role in this transformation. Interestingly, our catalyst is air-stable and can be recycled at least 5 times without losing catalytic activity.

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