95 research outputs found

    NUCLEIC-ACID BINDING-DRUGS .8. STRUCTURES OF 1-[2-(DIETHYLAMINO)ETHYLAMINO]ANTHRACENE-9,10-DIONE, C20H22N2O2 (I), AND 1,5-BIS[2-(DIETHYLAMINO)ETHYLAMINO]ANTHRACENE-9,10-DIONE, C26H36N4O2(II), MODELS FOR ANTI-TUMOR DRUGS

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    (I) M r = 322.41, P21/n, a = 7.118 (1), b = 26.873(2), c=8.886(1)A, fl=97.74(1)°, ~ V= 1684.3 (6) A 3, Z = 4, D m = 1.27, D x = 1.271 Mg m -3, 2 (Cu Ka) = 1.54178 A,/~ = 6.67 cm -1, F(000) = 688, T= 298 K, R w= 0.049 for 981 unique significant reflections. (II) Mr=436.61, P21/c, a= 15.360 (2), b = 5.245 (1), c= 15.483 (1)A, fl= 94.23 (1) °, V= 1244.0 (5)/~3, Z = 2, D m -- 1.17, D x = 1.165 Mg m -s, 2(Cu Kt~) = 1.54178/k, /t = 5.98 cm -1, F(000) = 472, T= 298 K, R w = 0.090 for 457 unique significant reflections. The chromophore is highly planar in both compounds

    STRUCTURE OF 2,3-DIHYDRO-1H-IMIDAZO[1,2-B]PYRAZOLE (IMPY), AN INHIBITOR OF DNA-SYNTHESIS, C5H7N3

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    Mr= 109.13, orthorhombic, P212121, a= 7.098 (1), b=7.225 (1), c= 10.980 (3)A, V= 563.09A 3, Z-4, D m=1.29, D x=l.29Mgm -a, 2(CuKs)=l.54178A, p=0.70mm -~. Final R= 0.059 for 425 significant reflections measured at 298 K. The pyrazole portion is planar, while the dihydroimidazole group has a shallow half-chair conformation with C(4) deviating by 0.136 (4) A out of the plane of this ring

    STRUCTURE OF 1-(PARA-METHOXYPHENYL)-TRANS-1,2-DIPHENYLBUT-1-ENE

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    C23H220 , triclinic, P1, a = 9.644 (3), b = 10.0001 (3), c = 10.4999 (3) A, c~ = 78.77 (3), fl = 67.53 (3), y= 74.91 (2) ° , V=898.3 A3, dc= 1.16 Mg m -3, Z = 2. There are two independent molecules in the asymmetric unit, which have very similar conformations. The structure was refined to a final R of 0.0586 for 2294 significant reflections

    MOLECULAR-MODELLING AND BIOPHYSICAL STUDIES ON MODIFIED AND UNMODIFIED OLIGONUCLEOTIDES

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    Computer graphics modelling and energy calculations have been carried out on a series of modified and unmodified oligonucleotides to investigate the effects of base deletion, base substitution and base methylation, particularly 06-methylguanine and 5-methylcytosine, as well as the substitution of bases by analogues

    Molecular-modelling and biophysical studies on modified and unmodified oligonucleotides

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    Idiopathic scoliosis and pineal lesions in Australian children

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    PURPOSE: To determine whether treatment of pineal lesions in children is associated with development of idiopathic scoliosis. METHODS: 38 boys and 10 girls with pineal lesions were identified. Their mean age at presentation was 10 years. The pineal pathology varied from cysts and epidermoid to teratoma, germinoma, pineocytoma, and glioblastoma. Treatment ranged from biopsy/extirpation to radiotherapy. RESULTS: 12 patients died. No scoliosis was found in any females or any of the deceased. Two boys had scoliosis: one had a 12-degree right upper thoracic curve with 32-degree kyphosis and the other had a 60-degree right thoracolumbar idiopathic curve, requiring a 2-stage arthrodesis. CONCLUSION: Pineal ablation is not related to the development of idiopathic scoliosis in humans

    Regulation of Motor Function and Behavior by Atypical Chemokine Receptor 1

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    The final publication is available at Springer via http://dx.doi.org/10.1007/s10519-014-9665-7Atypical Chemokine Receptor 1 (ACKR1), previously known as the Duffy Antigen Receptor for Chemokines, stands out among chemokine receptors for its high selective expression on Purkinje cells of the cerebellum, consistent with the ability of ACKR1 ligands to activate Purkinje cells in vitro. Nevertheless, evidence for ACKR1 regulation of brain function in vivo has been lacking. Here we demonstrate that Ackr1−/− mice have markedly impaired balance and ataxia when placed on a rotating rod and increased tremor when injected with harmaline, a drug that induces whole-body tremor by activating Purkinje cells. Ackr1−/− mice also exhibited impaired exploratory behavior, increased anxiety-like behavior and frequent episodes of marked hypoactivity under low-stress conditions. The behavioral phenotype of Ackr1−/− mice was the opposite of the phenotype occurring in mice with cerebellar degeneration and the defects persisted when Ackr1 was deficient only on non-hematopoietic cells. We conclude that normal motor function and behavior depend in part on negative regulation of Purkinje cell activity by Ackr1

    The International Limits and Population at Risk of Plasmodium vivax Transmission in 2009

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    Growing evidence shows that Plasmodium vivax malaria is clinically less benign than has been commonly believed. In addition, it is the most widely distributed species of human malaria and is likely to cause more illness in certain regions than the more extensively studied P. falciparum malaria. Understanding where P. vivax transmission exists and measuring the number of people who live at risk of infection is a fundamental first step to estimating the global disease toll. The aim of this paper is to generate a reliable map of the worldwide distribution of this parasite and to provide an estimate of how many people are exposed to probable infection. A geographical information system was used to map data on the presence of P. vivax infection and spatial information on climatic conditions that impede transmission (low ambient temperature and extremely arid environments) in order to delineate areas where transmission was unlikely to take place. This map was combined with population distribution data to estimate how many people live in these areas and are, therefore, exposed to risk of infection by P. vivax malaria. The results show that 2.85 billion people were exposed to some level of risk of transmission in 2009
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