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1.
Artigo em Inglês | MEDLINE | ID: mdl-25914900

RESUMO

BACKGROUND: There is concern that elders are not adequately evaluated prior to colon cancer surgery. We sought to determine adherence with ACOVE-3 (Assessing Care of Vulnerable Elders) quality indicators for pre-operative staging prior to colectomy for colon cancer utilizing the Surveillance, Epidemiology and End Results (SEER)-Medicare linked database (1992-2005). METHODS: We determined the proportion of patients aged 75 and older who had preoperative staging prior to colectomy for colon adenocarcinoma. Preoperative staging was defined as abdominopelvic computed tomography or magnetic resonance imaging scan (SCAN) and colonoscopy or flexible sigmoidoscopy (SCOPE). Multivariate logistic regression identified predictors of adherence. Odds ratios were adjusted for comorbidity, socioeconomic status, and disease severity. The association of adherence to ACOVE-3 and survival was quantified. RESULTS: Of the 37,862 patients, the majority were 75-84 years, 28% of the patients were ≥85 years. Regarding preoperative staging in the 6-month interval prior to surgical resection, 8% had neither SCAN nor SCOPE, 6% had only SCAN, 43% had only SCOPE, and 43% had both SCAN and SCOPE. Compared to patients who were not staged, those evaluated with either SCOPE alone or SCAN plus SCOPE had lower odds of 3-year mortality. Patients who were staged with SCAN alone had an increased odds of death compared to those who had neither SCAN or SCOPE. CONCLUSIONS: These data demonstrate that the majority of vulnerable elders with colon cancer did not receive appropriate preoperative staging prior to resection. The findings also confirm that adherence to ACOVE-3 guidelines is associated with improved long-term survival.

2.
J Med Chem ; 22(12): 1538-41, 1979 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-536998

RESUMO

The synthesis of 17-epi-ethynylestradiol (10), the 17 beta-ethynyl-17 alpha-ol epimer of the well-known orally active estrogen, ethynylestradiol (1), was achieved by LiA1H4 reduction of epoxide 9, as well as by demethylating epimestranol (11) with CH3MgI. Compound 11 was obtained by the unusual 17 beta-ethynylation of estrone 3-methyl ether 22 under equilibrating conditions. The in vitro estrogen receptor-binding affinity and the oral estrogenicity in the rat for the 17-epi compounds 10, 11 and 20 (epiquinestrol) was evaluated. Despite moderate estrogen receptor-binding affinity, compound 10 was devoid of measurable estrogenicity at 10 mg/kg or antiestrogenicity at 3 mg/kg.


Assuntos
Etinilestradiol/análogos & derivados , Etinilestradiol/síntese química , Mestranol/síntese química , Norpregnatrienos/síntese química , Quinestrol/síntese química , Animais , Antagonistas de Estrogênios/síntese química , Etinilestradiol/metabolismo , Etinilestradiol/farmacologia , Feminino , Técnicas In Vitro , Mestranol/metabolismo , Mestranol/farmacologia , Quinestrol/metabolismo , Quinestrol/farmacologia , Coelhos , Ratos , Receptores de Estrogênio/metabolismo , Estereoisomerismo , Útero/efeitos dos fármacos , Vagina/efeitos dos fármacos
3.
J Med Chem ; 20(12): 1546-51, 1977 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-592318

RESUMO

The preparation of a series of O-aryloximes of various steroids by two different routes is described. These compounds were prepared by reacting a keto steroid with a substituted O-arylhydroxylamine in the presence of an acid catalyst or, alternatively, by the reaction of a steroidal oxime with a substituted aryl halide in the presence of a suitable base. These compounds were examined for their ability to interrupt postimplantive gestation in female rats. The most significant contragestational activity was seen with compounds in which the basic steroid structure was a 5alpha-androstane and the 3-oxime was of the p-nitrophenyl series. One of the most active compounds in the series (16) was shown to have the ability to terminate pregnancy, when orally administered to rats at 2.5 mg/kg on days 9-12 of gestation. This compound was found to be devoid of androgenic activity at this dose level.


Assuntos
Oximas/síntese química , Prenhez/efeitos dos fármacos , Esteroides/síntese química , Animais , Feminino , Oximas/farmacologia , Gravidez , Ratos , Esteroides/farmacologia , Relação Estrutura-Atividade
5.
J Med Chem ; 16(2): 113-5, 1973 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-4683105

RESUMO

PIP: 3-aza-A-homo steroids have been of interest to these authors in their efforts to develop novel progestational agents. Because it exhibits antifertility activity both in humans and animals, 17alpha-ethynyl-19-nortestosterone (norethindrone) was chosen to undergo molecular modification. The syntheses of a number of oximino and 3-aza-A-homoandrostenes are described in the experimental section of the article. The progestational responses of the compounds were tested through the observation of rabbit uteri. The capacity of a compound to inhibit fertility in rate was noted from the minimum effective dose, i.e., the amount of compound in mg/kg per day which completely suppressed litter production (compound given to both male and female). Because of the suspicion that the oximino steroids were acting postcoitally, 17-beta-acetoxy-19-norandrost-4-en-3-one oxime was studied for its postcoital activity in rats. The postcoital antifertility action of the compound appears to be due to lytic degeneration of zygotes and/or their rapid expulsion from the reproductive tract. Some structure-function observations are made concerning the various compounds.^ieng


Assuntos
Androstenos/síntese química , Anticoncepcionais Pós-Coito/síntese química , Progestinas/síntese química , Androstenos/farmacologia , Animais , Compostos Aza/síntese química , Compostos Aza/farmacologia , Anticoncepcionais Pós-Coito/farmacologia , Feminino , Fertilidade/efeitos dos fármacos , Homosteroides/síntese química , Homosteroides/farmacologia , Noresteroides/síntese química , Noresteroides/farmacologia , Oximas/síntese química , Oximas/farmacologia , Progestinas/farmacologia , Coelhos , Ratos , Espectrofotometria Ultravioleta , Útero/efeitos dos fármacos
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