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Synthesis, SAR, and in Silico ADME Screening Studies of Some 9-Amino-3-Phenylacridone Derivatives as Topoisomerase II Inhibitors

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Open Journal of Medicinal Chemistry 2023年第2期13卷 15-34页

作者： Abiodun S. Oyedele Toluwase H. Fatoki esha dalvie Neil Osheroff Cosmas O. Okoro Department of Chemistry Tennessee State University Nashville Tennessee USA Applied Bioinformatics Laboratory Department of Biochemistry Federal University Oye-Ekiti Oye-Ekiti Nigeria Departments of Biochemistry Vanderbilt University School of Medicine Nashville Tennessee USA Medicine (Hematology/Oncology) Vanderbilt University School of Medicine Nashville Tennessee USA Vanderbilt Institute of Chemical Biology Vanderbilt University School of Medicine Nashville Tennessee USA

Cancer is a leading cause of death globally, claiming about 9.6 million lives and approximately 420 million new cases of cancer will be diagnosed in the world by the year 2025. The aim of this study was to synthesize and computationally evaluate pharmacological potential of some derivatives of 9-amino-3-phenylacridone, as topoisomerase II (Topo II) inhibitors. In this study, 10 derivatives of 3-phenyl-9-aminoacridone were chemically synthesized and characterized, and the potential pharmacological indications of these compounds were computationally predicted by methods such as ADMET prediction, molecular target prediction and molecular docking. The results showed that two derivatives (58e and 58j) were non-permeant of blood-brain barrier, and this property was found similar to that of amsacrine and etoposide. The results of molecular docking of the ten derivatives of 3-phenyl-9-aminoacridone that were synthesized in this work showed that the synthetic compounds (58a-j) and the standard drugs have overall best binding affinities for human acetylcholine esterase than butyrylcholinesterase, and overall best binding affinities for human topo IIα than human topo IIβ. Overall, the results of this study suggest that the synthetic compounds 58a, 58c, 58f, 58g, and 58i could probably inhibit topo IIα by catalytic inhibition as seen with amsacrine, but only 58b and 58e possessed DNA non-intercalation properties as seen with etoposide, serving as topo II poison. In conclusion, this study showed that 3-phenyl-9-aminoacridone derivatives are potential inhibitor of topo IIα/β both by catalytic inhibition and poison as non-intercalator of DNA.

关键词： Cancers 9-Aminoacridone Anticancer Topoisomerase II Pharmacokinetics Molecular Docking Etoposide

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Manubriosternal dislocation with spinal fracture： A rare cause for delayed haemothorax

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Chinese Journal of Traumatology 2015年第4期18卷 245-248页

作者： Manish Kothari Pramod Saini Sunny Shethna Samir dalvie Spine Room 1408. Hinduja Clinic PD Hinduja National Hospital & MRC Mahim Mumbai Maharashtra 400016 India

Type 2 manubriosternal dislocations with concomitant spinal fracture are rare and may be associated with thoracic visceral injuries. The complication of delayed haemothorax has not been reported yet. We report a case of a young male who suffered manubriosternal dislocation with chance type thoracic spine fracture due to fall of a tree branch over his back. The haemothorax presented late on day three. The possible injury mechanism is discussed along with review of literature. We conclude that a lateral chest radiograph is indicated in spinal fracture patients complaining of midsternal pain. Computerized axial tomography scan of chest with contrast is indicated to rule out visceral injuries and a chest radiograph should be repeated before the patient is discharged to look for delayed haemothorax.

关键词： Manubriosternal dislocation Spinal fractures Haemothorax

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Understanding diarrhoeal diseases in response to climate variability and drought in Cape Town, South Africa: a mixed methods approach

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Infectious Diseases of Poverty 2023年第4期12卷 105-105页

作者： Tristan Taylor Lee Mohamed Aqiel dalvie Martin Röösli Sonja Merten Marek Kwiatkowski Hassan Mahomed Neville Sweijd Guéladio Cissé Swiss Tropical and Public Health Institute Allschwil Switzerland University of Basel Basel Switzerland Centre for Environmental and Occupational Health Research School of Public Health University of Cape Town Cape Town South Africa Metro Health Services Western Cape Government: Health and Wellness Western Cape South Africa Division of Health Systems and Public Health Department of Global Health Faculty of Medicine and Health Sciences Stellenbosch University Stellenbosch South Africa Alliance for Collaboration on Climate and Earth Systems Science Council for Scientific and Industrial Research Pretoria South Africa

BackgroundThe climate of southern Africa is expected to become hotter and drier with more frequent severe droughts and the incidence of diarrhoea to increase. From 2015 to 2018, Cape Town, South Africa, experienced a severe drought which resulted in extreme water conservation efforts. We aimed to gain a more holistic understanding of the relationship between diarrhoea in young children and climate variability in a system stressed by water *** a mixed-methods approach, we explored diarrhoeal disease incidence in children under 5 years between 2010 to 2019 in Cape Town, primarily in the public health system through routinely collected diarrhoeal incidence and weather station data. We developed a negative binomial regression model to understand the relationship between temperature, precipitation, and relative humidity on incidence of diarrhoea with dehydration. We conducted in-depth interviews with stakeholders in the fields of health, environment, and human development on perceptions around diarrhoea and health-related interventions both prior to and over the drought, and analysed them through the framework *** diarrhoeal incidence data, the diarrhoea with dehydration incidence decreased over the decade studied, e.g. reduction of 64.7% in 2019 [95% confidence interval (CI): 5.5–7.2%] compared to 2010, with no increase during the severe drought period. Over the hot dry diarrhoeal season (November to May), the monthly diarrhoea with dehydration incidence increased by 7.4% (95% CI: 4.5–10.3%) per 1 °C increase in temperature and 2.6% (95% CI: 1.7–3.5%) per 1% increase in relative humidity in the unlagged model. Stakeholder interviews found that extensive and sustained diarrhoeal interventions were perceived to be responsible for the overall reduction in diarrhoeal incidence and mortality over the prior decade. During the drought, as diarrhoeal interventions were maintained, the expected increase in incidence in the public health sector di

关键词： routine drought humidity

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