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1.
Bioorg Med Chem ; 19(6): 1950-8, 2011 Mar 15.
Artículo en Inglés | MEDLINE | ID: mdl-21353569

RESUMEN

Xanthine oxidase is a complex molybdoflavoprotein that catalyses the hydroxylation of xanthine to uric acid. Fifty three analogues of 1-acetyl-3,5-diaryl-4,5-dihydro(1H)pyrazoles were rationally designed and synthesized and evaluated for in vitro xanthine oxidase inhibitory activity for the first time. Some notions about structure activity relationships are presented. Six compounds 41, 42, 44, 46, 55 and 59 were found to be most active against XO with IC(50) ranging from 5.3 µM to 15.2 µM. The compound 59 emerged as the most potent XO inhibitor (IC(50)=5.3 µM). Some of the important interactions of 59 with the amino acid residues of active site of XO have been figured out by molecular modeling.


Asunto(s)
Inhibidores Enzimáticos/síntesis química , Pirazoles/química , Xantina Oxidasa/antagonistas & inhibidores , Sitios de Unión , Dominio Catalítico , Simulación por Computador , Diseño de Fármacos , Inhibidores Enzimáticos/química , Inhibidores Enzimáticos/farmacología , Isomerismo , Pirazoles/síntesis química , Pirazoles/farmacología , Relación Estructura-Actividad , Xantina Oxidasa/metabolismo
2.
Anticancer Res ; 37(10): 5609-5616, 2017 10.
Artículo en Inglés | MEDLINE | ID: mdl-28982877

RESUMEN

BACKGROUND/AIM: The purpose of this study was to prove the effect of complete surgical staging of patients with mucinous borderline ovarian tumors (mBOTs) especially appendectomy on progression-free survival (PFS) and overall survival (OS). PATIENTS AND METHODS: The database of 14 gynecological oncology departments from Turkey and Germany were comprehensively searched for women who underwent primary surgery for an ovarian tumor between January 1, 1998, and December 31, 2015, and whose final diagnosis was mBOT. RESULTS: A total of 364 patients with mBOT with a median age of 43.1 years were included in this analysis. The median OS of all patients was 53.1 months. The majority of cases had Stage IA (78.6%). In univariate and multivariate analyses, radical surgery, omentectomy, appendectomy, lymphadenectomy, and adding adjuvant chemotherapy were not independent prognostic factors for PFS and OS. Furthermore, FIGO stage (≥IC vs.

Asunto(s)
Procedimientos Quirúrgicos Ginecológicos , Estadificación de Neoplasias/métodos , Neoplasias Quísticas, Mucinosas y Serosas/patología , Neoplasias Quísticas, Mucinosas y Serosas/cirugía , Neoplasias Ováricas/patología , Neoplasias Ováricas/cirugía , Adolescente , Adulto , Anciano , Anciano de 80 o más Años , Apendicectomía , Quimioterapia Adyuvante , Progresión de la Enfermedad , Supervivencia sin Enfermedad , Femenino , Alemania , Procedimientos Quirúrgicos Ginecológicos/efectos adversos , Procedimientos Quirúrgicos Ginecológicos/mortalidad , Humanos , Estimación de Kaplan-Meier , Escisión del Ganglio Linfático , Persona de Mediana Edad , Análisis Multivariante , Neoplasias Quísticas, Mucinosas y Serosas/mortalidad , Neoplasias Ováricas/mortalidad , Valor Predictivo de las Pruebas , Modelos de Riesgos Proporcionales , Estudios Retrospectivos , Factores de Riesgo , Factores de Tiempo , Resultado del Tratamiento , Turquía , Adulto Joven
3.
J Ovarian Res ; 9(1): 66, 2016 Oct 18.
Artículo en Inglés | MEDLINE | ID: mdl-27756415

RESUMEN

BACKGROUND: The optimal surgical management and staging of borderline ovarian tumors (BOTs) are controversial. Institutions have different surgical approaches for the treatment of BOTs. Here, we performed a retrospective review of clinical characteristics, surgical management and surgical outcomes, and sought to identify variables affecting disease-free survival (DFS) and overall survival (OS) in patients with BOTs. METHODS: A retrospective review of ten gynecological oncology department databases in Turkey was conducted to identify patients diagnosed with BOTs. The effects of type of surgery, age, stage, surgical staging, complete versus incomplete staging, and adjuvant chemotherapy were examined on DFS and OS. RESULTS: In total, 733 patients with BOTs were included in the analysis. Most of the staged cases were in stage IA (70.4 %). In total, 345 patients underwent conservative surgeries. Recurrence rates were similar between the conservative and radical surgery groups (10.5 % vs. 8.7 %). Furthermore we did not find any difference between DFS (HR = 0.96; 95 % confidence interval, CI = 0.7-1.2; p = 0.576) or OS (HR = 0.9; 95 % CI = 0.8-1.1; p = 0.328) between patients who underwent conservative versus radical surgeries. There was also no difference in DFS (HR = 0.74; 95 % CI = 0.8-1.1; p = 0.080) or OS (HR = 0.8; 95 % CI = 0.7-1.0; p = 0.091) between complete, incomplete, and unstaged patients. Furthermore, receiving adjuvant chemotherapy (CT) for tumor stage ≥ IC was not an independent prognostic factor for DFS or OS. CONCLUSIONS: Patients undergoing conservative surgery did not show higher recurrence rates; furthermore, survival time was not shortened. Detailed surgical staging, including lymph node sampling or dissection, appendectomy, and hysterectomy, were not beneficial in the surgical management oF BOTs.


Asunto(s)
Neoplasias Ováricas/diagnóstico , Adulto , Biopsia , Terapia Combinada , Manejo de la Enfermedad , Femenino , Humanos , Estimación de Kaplan-Meier , Persona de Mediana Edad , Clasificación del Tumor , Recurrencia Local de Neoplasia , Estadificación de Neoplasias , Neoplasias Ováricas/mortalidad , Neoplasias Ováricas/terapia , Retratamiento , Estudios Retrospectivos , Resultado del Tratamiento , Ultrasonografía , Adulto Joven
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