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MP Costi D Tondi M Rinaldi D Barlocco G Cignarella DV Santi C Musiu I Pudu G Vacca P La Colla 《European journal of medicinal chemistry》1996,31(12):1011-1016
A new series of N-(substituted)benzyl-1,8-naphthalimides 4, structurally related to the previously reported thymidylate synthase (TS) inhibitor naphthaleins 3, were synthesized and compounds tested for their inhibition of several species of TS. Moreover, their in vitro cytotoxicity together with antimycotic and antibacterial properties were assayed. While no activity was detected in the antibacterial tests, the m-nitro (4ae) and the p-nitro (4af) derivatives were found able to partially inhibit TS at low micromolar concentrations. Introduction of nitro or (substituted)-amino groups in position 4 of the naphthalic ring always led to less active compounds. 相似文献
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Tortoriello DV; McGovern PG; Colon JM; Loughlin J; Santoro N 《Human reproduction (Oxford, England)》1998,13(11):3005-3008
We report an instance of critical ovarian hyperstimulation syndrome in a
highly responsive in-vitro fertilization patient despite the preventive
measure of a 4 day 'coast' interval during which no gonadotrophins were
administered while gonadotrophin-releasing hormone agonist therapy
continued until serum oestradiol concentrations fell below 3000 pg/ml.
相似文献
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L Ozzello CM De Rosa EW Blank K Cantell RL Ceriani DV Habif Sr 《Breast cancer research and treatment》1993,25(3):265-276
Summary An immunoconjugate composed of natural interferon (nIFN) bound in a noncleavable fashion to a monoclonal antibody (MoAb) recognizing a breast epithelial membrane mucin (Mc5) was used to treat xenografts of a human mammary carcinoma cell line (MCF-7) growing in nude mice. The immunoconjugate (nIFN/Mc5) was administered as 20 intralesional (i.l.) injections to 1 of 2 xenografts in each animal. It was found that nIFN/Mc5 produced a significant enhancement of the growth inhibitory actions of nIFN on the injected tumors. Further enhancement was obtained when nIFN or nIFN together with Mc5 (at a dose 10 times larger than that present in nIFN/Mc5) were added to the immunoconjugate. Biodistribution experiments showed that the uptake of125I-nIFN/Mc5 by the tumors was greater and its elimination slower than for125I-nIFN alone or conjugated to irrelevant mouse IgG1. In addition, the immunoconjugate up-regulated the antigenic expression of a breast epithelial membrane mucin by the carcinoma cells, an up-regulation which was not significantly different from that produced by nIFN alone. The contralateral noninjected tumors exposed to systemic levels of the immunoconjugate showed an enhancement of antitumor effects, but to a lesser extent than the injected tumors. These findings suggest that the enhancement of the growth inhibitory action of the immunoconjugate was related to the specific binding of Mc5 which targeted the IFN to the carcinoma cells and impeded its elimination. It is likely that the targeting was favored by the IFN-mediated up-regulation of antigenic expression by the carcinoma cells, thereby producing a cascade of interrelated effects. The results of this study point out the feasibility and potential usefulness of IFN treatment by means of immunoconjugates as well as the worth of pursuing and improving this form of therapy. 相似文献
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The effect of combined treatment with nitrosorbide and obsidan on major hemodynamic parameters was studied in 47 myocardial infarction patients within the first 24 hours of the disease. Intravenous drip injection of 0.15 mg/kg obsidan simultaneously with the administration of 20 mg nitrosorbide reduced heart rate by 12.7%, systemic blood pressure by 23.5%, and diastolic pulmonary arterial pressure by 38.4%. The cardiac index decreased by 22.8%, mainly due to reduced heart rate. The treatment improved myocardial function as evidenced by and increased number of positive post-treatment "functional curves". This method is safe and efficient, provided it is applied under careful hemodynamic control. 相似文献
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A 4 year old girl with neurofibromatosis type 1 (NF1) was referred for hypertension. An aortogram showed narrowing of the left main renal artery. An angiogram three and a half years later showed coarctation of the abdominal aorta. She underwent aortoplasty but the stenosis recurred. Vascular involvement in NF1 may be progressive and requires long term follow up. 相似文献
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The foramen ovale is usually obliterated following establishment of the adult circulation but remains patent in 25% of individuals. This potential communication between the venous and arterial circulations can allow thromboembolic material to bypass the lungs and enter the systemic circulation. We report two cases of paradoxical embolization through a patent foramen ovale following acute large pulmonary embolism (PE) and discuss the factors that predispose to paradoxical embolization following PE. 相似文献
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