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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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The synthesis of polymers of intrinsic microporosity (PIMs)

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Science China Chemistry 2017年第8期60卷 1023-1032页

作者： neil B.McKeown School of Chemistry University of Edinburgh David Brewster Road Edinburgh EH9 3F J U

Polymers of intrinsic microporosity （PIMs） are a class of porous organic polymer （POP） that form microporous solids due to the inefficient packing of their rigid and contorted macromolecular chains. In contrast to other types of POP, PIMs are not comprised of a network of cross-linked covalent bonds so that they can be dissolved in organic solvents and processed into robust films, coatings or fibres. Here, over twelve years＇ accumulated research on the synthesis of PIMs is reviewed. To date, three types of polymerisation reaction have been used successfully to prepare PIMs of sufficient molecular mass to form robust self-standing films. These involve the formation of dibenzodioxin, Tr6ger＇s base and imide linkages between monomeric units. This rapid development of synthetic methods for preparing PIMs has been driven by their rich potential for numerous diverse applications and this synergistic relationship between synthesis and functionality is set to continue.

关键词： polymers of intrinsic microporosity synthesis porous organic polymers

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Hyperhomocysteinemia, endoplasmic reticulum stress, and alcoholic liver injury

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World Journal of Gastroenterology 2004年第12期10卷 1699-1708页

作者： neil Kaplowitz Gastroenterology/Liver Division Keck School of MedicineUniversity of Southern CaliforniaLos AngelesCA 90033USA

Deficiencies in vitamins or other factors(B6,B12,folic acid, betaine)and genetic disorders for the metabolism of the non-protein amino acid-homocysteine(Hcy)lead to hyperhomocysteinemia(HHcy).HHcy is an integral component of several disorders including cardiovascular disease,neurodegeneration,diabetes and alcoholic liver *** unleashes mediators of inflammation such as NFκB,IL-1β,IL-6,and IL-8,increases production of intracellular superoxide anion causing oxidative stress and reducing intracellular level of nitric oxide(NO),and induces endoplasrnic reticulum(ER)stress which can explain many processes of Hcy-promoted cell injury such as apoptosis, fat accumulation,and *** models have played an important role in determining the biological effects of *** stress may also be involved in other liver diseases such as α_1-antitrypsin(α_1-AT)deficiency and hepatitis C and/or B virus *** research should evaluate the possible potentiative effects of alcohol and hepatic virus infection on ER stress-induced liver injury,study potentially beneficial effects of lowering Hcy and preventing ER stress in alcoholic humans,and examine polymorphisrn of Hcy metabolizing enzymes as potential risk-factors for the development of HHcy and liver disease.

关键词： Animals Endoplasmic Reticulum Humans Hyperhomocysteinemia Liver Diseases, Alcoholic Oxidative Stress

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No evidence of Permacol rejection presented by Wotton and Akoh

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World Journal of Gastroenterology 2010年第5期16卷 657-658页

作者： neil James Smart Department of General Surgery Royal Devon&Exeter HospitalBarrack RoadExeterEX2 5DW United Kingdom

Wotton and Akoh in their previously reported case in this journal postulate that Permacol *** letter provides a detailed critique of that claim and provides an alternative explanation for the histological data provided by the *** is also argued that Wotton and Akoh have misrepresented one of the papers in the discussion in their article and a clarification of that referenced paper is given.

关键词： Porcine dermal collagen implant(Permacol) Renal Transplant Rejection

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Gamma-ray bursts in the swift-Fermi era

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Frontiers of physics 2013年第6期8卷 661-678页

作者： neil Gehrels Soebur Razzaque Astrophysics Science Division NASA Goddard Space Flight Center Greenbelt MD 20771 USA George Mason University Fairfax VA 22030 USA Resident at Space Science Division Naval Research Laboratory Washington DC 20375 USA

Gamma-ray bursts （GRBs） are among the most violent occurrences in the universe. They are pow- erful explosions, visible to high redshift, and thought to be the signature of black hole birth. They are highly luminous events and provide excellent probes of the distant universe. GRB research has greatly advanced over the past 10 years with the results from Swift, Fermi and an active followup community. In this review we survey the interplay between these recent observations and the theoretical models of the prompt GRB emission and the subsequent afterglows.

关键词： gamma-ray bursts (GRBs) Swift Fermi

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Relative abundance of American badger (Taxidea taxus) and red fox (Vulpes vulpes) in landscapes with high and low rodenticide poisoning levels

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Integrative Zoology 2012年第1期7卷 41-47页

作者： Gilbert PROULX neil MacKENZIE Alpha Wildlife Research&Management Sherwood ParkAlbertaCanada

Over the past decade,extensive poisoning campaigns have been conducted in southern Saskatchewan to control Richardson’s ground squirrel Spermophilus richardsonii(Sabine,1822)*** campaigns might impact on predator abundance by decreasing prey levels,and also through secondary *** spotlighting,we investigated the relative abundance of American badgers Taxidea taxus(Schreber,1777)and red fox Vulpes vulpes(Linnaeus,1758)in 2 study areas with road access and crops,but with different levels of *** the study area with relatively low poisoning(19.6%of the area traversed by roads),there were 2.2 times more American badgers per km of road and 6.4 times more red foxes per km than in the study area with high poisoning(89.7%of the area).It is recommended that an Integrated Pest Management program be developed to conserve natural predators across landscapes.

关键词： ground squirrels poisoning populations predators

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Herb-Induced Liver Injury: A Global Concern

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Chinese Journal of Integrative Medicine 2018年第9期24卷 643-644页

作者： neil Kaplowitz USC Research Center for Liver Disease USC Keck School of Medicine

Chinese medicine and herb medicine though used to treat liver diseases are an important cause of liver injury. Many phytochemicals have the potential to injure the liver, some in a dose-related fashion and more often in an idiosyncratic fashion, meaning occurrence is uncommon to rare in the population using these treatments. As is the case with pharmaceuticals, the phytochemicals are usually tolerated despite either no or mild transient subclinical injury but rarely in some susceptible patients cause moderate to severe liver injury which is likely mediated by the adaptive immune system.

关键词： herb-induced liver injury diagnosis and management guideline Chinese medicine

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Multimodality treatment of potentially curative gastric cancer: Geographical variations and future prospects

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World Journal of Gastroenterology 2014年第36期20卷 12892-12899页

作者： neil D Merrett Discipline of Surgery School of Medicine University Of Western Sydney Penrith NSW 2751 Australia Department of Upper Gastrointestinal Surgery Sydney South West Local Health District Liverpool NSW 2170 Australia

After much controversy, multimodality therapy is now accepted worldwide as the gold standard for treatment of resectable bulky localized gastric cancer. There is significant regional variation in the style of multimodality treatment with adjuvant chemoradiation the North American standard, neoadjuvant chemotherapy preferred in Europe and Australasia, whilst adjuvant chemotherapy is preferred in Asia. With further standardization of surgery and D1+/D2 resections increasingly accepted world wide, and in particular in the West, as the surgical standard of care for potentially curable disease, it is timely to reassess the multimodality regimes being used. The challenge in the use of multimodality therapy is how current outcomes can be standardized and improved further. Recent studies indicate that mere intensification of the regime in time, dosage or addition of further agents does not improve localized gastric cancer outcomes. More novel strategies including early commencement of adjuvant therapies, intra-peritoneal chemotherapy or assessing neoadjuvant response with positron emission tomography scanning may give improvements in outcomes. The introduction of targeted therapies means that the adjuvant use of biological agents needs to be explored. By proper assessment of the patient’s co-morbidities, full tumour staging, and a better understanding of the tumour’s molecular pathology, multimodality therapy for gastric adenocarcinoma may be individualized to optimize the likelihood of cure.

关键词： Gastric cancer Gastrectomy Multimodality Adjuvant treatment Neoadjuvant Targeted therapy Human epidermal growth factor receptor

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The effects of acquired paternal obesity on the next generation

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Asian Journal of Andrology 2011年第2期13卷 195-196页

作者： neil A Youngson Emma Whitelaw Queensland Institute of Medical Research 300 HerstonRoad Herston Brisbane 4006 Australia

It is well established that the health of mothers can influence the health of theiroffspring, i ms can occur as a result or me transfer of viruses or toxins via the placenta or the milk, a compromised nutrient supply to the embryo or abnormal behavioural inter- actions between mother and offspring） However, examples of paternal health affecting the next generation are rare.

关键词： Mothers Health Rats Milk Administration Managers Males

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Historical overview and review of current day treatment in the management of acute variceal haemorrhage

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World Journal of Gastroenterology 2014年第21期20卷 6481-6494页

作者： neil Rajoriya Dhiraj Tripathi Department of Hepatology The New Queen Elizabeth HospitalBirmingham B15 2THUnited Kingdom

Variceal haemorrhage is one of the most devastating consequences of portal hypertension, with a 1-year mortality of 40%. With the passage of time, acute management strategies have developed with improved survival. The major historical treatment landmarks in the management of variceal haemorrhage can be divided into surgical, medical, endoscopic and radiological breakthroughs. We sought to provide a historical overview of the management of variceal haemorrhage and how treatment modalities over time have impacted on clinical outcomes. A PubMed search of the following terms: portal hypertension, variceal haemorrhage, gastric varices, oesophageal varices, transjugular intrahepatic portosystemic shunt was performed. To complement this, Google™ was searched with the aforementioned terms. Other relevant references were identified after review of the reference lists of articles. The review of therapeutic advances was conducted divided into pre-1970s, 1970/80s, 1990s, 2000-2010 and post-2010. Also, a summary and review on the pathophysiology of portal hypertension and clinical outcomes in variceal haemorrhage was performed. Aided by the development of endoscopic therapies, medication and improved radiological interventions; the management of variceal haemorrhage has changed over recent decades with improved survival from an often-terminating event in recent past.

关键词： Variceal haemorrhage Oesophageal varices Gastric varices Portal hypertension

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