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1.
J Asian Nat Prod Res ; 26(3): 342-352, 2024 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-37933140

RESUMO

Bicyclol, an innovative hepatoprotective drug, was approved by the Chinese National Medical Products Administration (NMPA) in 2001 to treat Hepatitis B and drug-induced liver injury. Two active metabolites of bicyclol have been identified as M2 and M3. To evaluate the impact on drug safety and efficacy of possible drug-drug interactions (DDIs) associated with these metabolites, a sufficient quantity of these metabolites is required. Herein, we report a concise novel route for the synthesis of M2 and M3 using the Suzuki-Miyaura coupling as the key step. Furthermore, we complete the gram-scale syntheses of M2 and M3.


Assuntos
Compostos de Bifenilo , Doença Hepática Induzida por Substâncias e Drogas , Compostos de Bifenilo/farmacologia , Substâncias Protetoras , Doença Hepática Induzida por Substâncias e Drogas/tratamento farmacológico
2.
World J Gastroenterol ; 11(19): 2927-31, 2005 May 21.
Artigo em Inglês | MEDLINE | ID: mdl-15902730

RESUMO

AIM: To investigate if non-peptidic small molecular inhibitors of the p53-HDM2 interaction could restore p53 function and kill tumor cells. METHODS: A series of non-peptidic small HDM2 inhibitors were designed by computer-aided model and synthesized by chemical method. Syl-155 was one of these inhibitors. Cytotoxic effect of syl-155 on three tumor cell lines with various states of p53, HT1080 (wild-type p53), KYSE510 (mutant p53), MG63 (p53 deficiency) was evaluated by MTT assay, Western blot and flow cytometry. RESULTS: Syl-155 stimulated the accumulation of p53 and p21 protein in HT1080 cells expressing wild-type p53, but not in KYSE510 and MG63 cells. Consequently, syl-155 induced cell cycle arrest and apoptosis in HT1080 cells. CONCLUSION: Non-peptidic small molecular inhibitors of the p53-HDM2 interaction show promise in treatment of tumors expressing wild-type p53.


Assuntos
Apoptose/efeitos dos fármacos , Carcinoma de Células Escamosas , Neoplasias Esofágicas , Proteínas Nucleares/metabolismo , Peptídeos/farmacologia , Proteínas Proto-Oncogênicas/metabolismo , Proteína Supressora de Tumor p53/metabolismo , Neoplasias Ósseas , Divisão Celular/efeitos dos fármacos , Linhagem Celular Tumoral , Sobrevivência Celular/efeitos dos fármacos , Citotoxinas/farmacologia , Fibrossarcoma , Humanos , Proteínas Nucleares/genética , Osteossarcoma , Proteínas Proto-Oncogênicas/genética , Proteínas Proto-Oncogênicas c-mdm2 , Proteína Supressora de Tumor p53/genética
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