RESUMEN
The design, synthesis, and DNA binding properties of azaHx-PI or p-anisyl-4-aza-benzimidazole-pyrrole-imidazole (5) are described. AzaHx, 2-(p-anisyl)-4-aza-benzimidazole-5-carboxamide, is a novel, fluorescent DNA recognition element, derived from Hoechst 33258 to recognize G·C base pairs. Supported by theoretical data, the results from DNase I footprinting, CD, ΔT(M), and SPR studies provided evidence that an azaHx/IP pairing, formed from antiparallel stacking of two azaHx-PI molecules in a side-by-side manner in the minor groove, selectively recognized a C-G doublet. AzaHx-PI was found to target 5'-ACGCGT-3', the Mlu1 Cell Cycle Box (MCB) promoter sequence with specificity and significant affinity (K(eq) 4.0±0.2×10(7) M(-1)).
Asunto(s)
Bencimidazoles/química , ADN/metabolismo , Colorantes Fluorescentes/química , Nylons/química , Pirroles/química , Antígenos de Neoplasias/genética , Antígenos de Neoplasias/metabolismo , Emparejamiento Base , Bencimidazoles/síntesis química , Bencimidazoles/metabolismo , Sitios de Unión , Técnicas de Química Sintética , Dicroismo Circular , ADN/química , ADN-Topoisomerasas de Tipo II/genética , ADN-Topoisomerasas de Tipo II/metabolismo , Proteínas de Unión al ADN/genética , Proteínas de Unión al ADN/metabolismo , Desoxirribonucleasa I/química , Diseño de Fármacos , Colorantes Fluorescentes/metabolismo , Nylons/síntesis química , Regiones Promotoras Genéticas , Pirroles/síntesis química , Pirroles/metabolismoRESUMEN
Two divergent series of novel chalcone analogs, one derived from 1-cyclohexylpyrrolidin-2-one and the other derived from 1-benzo[f]chromanone, were designed, synthesized and evaluated for cytotoxicity against two murine cancer cell lines. Two 1-benzo[f]chromanone analogs, 4g and 4j yielded moderate toxicity against both melanoma B16 and lymphoma L1210 cell lines with IC(50) values between the range of 5 and 6 µM. With an IC(50) value of 3.4 µM, compound 4g was also active against human MDA-MB-435 melanoma cells. X-ray structures of the ß-hydroxy ketone product (4a) and the α,ß-unsaturated ketone (4h) were collected, and confirm the syn-configuration between the carbonyl moiety and the ß-vinylic proton in 4h. X-ray structures of two 1-cyclohexylpyrrolidin-2-one derivatives were also obtained, and both showed an E-configuration for the double bond.
Asunto(s)
Antineoplásicos/síntesis química , Chalconas/síntesis química , Cromonas/química , Ciclohexanos/química , Pirrolidinonas/química , Animales , Antineoplásicos/farmacología , Línea Celular Tumoral , Supervivencia Celular/efectos de los fármacos , Chalconas/química , Chalconas/farmacología , Diseño de Fármacos , Humanos , Ratones , Relación Estructura-Actividad , Difracción de Rayos XRESUMEN
The synthesis and full characterization (mp, NMR, UV/vis, FTIR, and elemental analysis) of 13 bismuth aryloxides are reported. We have prepared bismuth aryloxides with alkyl, aryl, and allylic substituents on the aryl rings. Eleven of these bismuth aryloxides have been characterized with single crystal X-ray diffraction methods. Bismuth-donor interactions (donor = aryl, methoxy) are observed in several cases. Three unexpected bismuth oxo aryloxides (6c, 9c, 11c) were also isolated. Complex C(77)H(102)Bi(4)Br(6)O(8) (6c) results from apparent C-H activation and Bi-C bond formation as a sideproduct in the synthesis of Bi(O-2,6-(i)Pr(2)-4-BrC(6)H(2))(3) (6). Cluster 9c has a Bi(32)O(56) core, and cluster C(90)H(90)Bi(4)Li(2)O(12) (11c) is the second lithium bismuth oxo cluster reported to date.
RESUMEN
The purpose of this study was to evaluate the therapeutic efficacy of the cooking group from the burn survivors' perspective. By incorporating concepts of kitchen skills, energy conservation, and desensitization techniques, the cooking group can assist patients with the functional use of their hands, standing tolerance, return to former vocational activities, and socialization with other patients. A questionnaire was developed based on commonly expressed benefits of cooking group. Areas of interest included decreasing anxiety in the kitchen, distraction from their burns, socializing with other burn survivors, and the physical benefits of participating in the group. The results of this study indicate that participants regard the therapeutic cooking group as a valuable treatment modality that effectively combines functional activities with socialization to decrease burn related anxiety and increase motion in a supportive environment for patients with burns.
Asunto(s)
Quemaduras/psicología , Quemaduras/rehabilitación , Culinaria , Procesos de Grupo , Terapia Ocupacional/métodos , Adulto , Anciano , Ansiedad/psicología , Ansiedad/rehabilitación , Miedo/psicología , Femenino , Humanos , Relaciones Interpersonales , Masculino , Persona de Mediana Edad , Encuestas y CuestionariosRESUMEN
The purpose of this study was to analyze the impact of a standard, custom-made pressure glove vs The NewYork-Presbyterian Dexterity Glove (NYPDG) with silon application on the palmer surface on functional hand use of burn survivors. A standard, custom-made pressure glove and NYPDG were given to 18 participants in a randomized order. Subjects wore each glove for 7 to 10 days during all activities of daily living (ADL). Variables such as hand function, difficulty of fine and gross motor ADL, and participant glove preference were assessed with each glove condition. Data collection of the second glove took place 7 to 10 days later incorporating a quasiexperimental, repeated measure design. A crossover design was used to analyze the data. The NYPDG demonstrated significantly better results in all of the four outcome categories measured: time to complete the Jebsen, the Jebsen Likert scale, fine motor ADL, and gross motor ADL. This study demonstrated that functional tasks took less time to complete and were more easily performed when using the NYPDG.
Asunto(s)
Actividades Cotidianas , Quemaduras/rehabilitación , Guantes Protectores , Traumatismos de la Mano/rehabilitación , Adulto , Anciano , Vendajes , Estudios Cruzados , Diseño de Equipo , Femenino , Humanos , Masculino , Persona de Mediana Edad , Satisfacción del Paciente , PresiónRESUMEN
The purpose of this study was to examine functional hand use in uninjured adults when wearing a standard, custom-made pressure glove (SPG) as compared with a glove with select placement of suede, The New York-Presbyterian Dexterity Glove (NYPDG) (patent pending). Thirty-four participants received a custom SPG and NYPDG in a randomized order. Gloves were worn for one day during all activities of daily living (ADL). Hand function, difficulty of fine and gross motor ADL, and participant glove preference were assessed. The process was repeated approximately 1 week later with the remaining glove incorporating a quasi-experimental, repeated measure design. Data were analyzed using a crossover design. Results were significant in favor of the NYPDG in all of the four outcome categories: time to complete the Jebsen, the Jebsen Likert scale, fine motor ADL, and gross motor ADL. In conclusion, this study demonstrated that functional tasks were faster and easier to perform when using the NYPDG.