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91.  Synthesis, antimicrobial evaluation, DNA gyrase inhibition, and in silico pharmacokinetic studies of novel quinoline derivatives.LinkIT
El-Shershaby MH, El-Gamal KM, Bayoumi AH, El-Adl K, Ahmed HEA, Abulkhair HS
Archiv der Pharmazie Arch Pharm (Weinheim) Synthesis, antimicrobial evaluation, DNA gyrase inhibition, and in silico pharmacokinetic studies of novel quinoline derivatives. e2000277 10.1002/ardp.202000277 Herein, we report the synthesis and in vitro antimicrobial evaluation of novel quinoline derivatives as DNA gyrase inhibitors. The preliminary antimicrobial activity was assessed against a panel of pathogenic microbes including Gram-positive bacteria (Streptococcus pneumoniae and Bacillus subtilis), Gram-negative bacteria (Pseudomonas aeruginosa and Escherichia coli), and fungal strains (Aspergillus fumigatus, Syncephalastrum racemosum, Geotrichum candidum, and Candida albicans). Compounds that revealed the best activity were subjected to further biological studies to determine their minimum inhibitory concentrations (MICs) against the selected pathogens as well as their in vitro activity against the E. coli DNA gyrase, to realize whether their antimicrobial action is mediated via inhibition of this enzyme. Four of the new derivatives (14, 17, 20, and 23) demonstrated a relatively potent antimicrobial activity with MIC values in the range of 0.66-5.29??g/ml. Among them, compound 14 exhibited a particularly potent broad-spectrum antimicrobial activity against most of the tested strains of bacteria and fungi, with MIC values in the range of 0.66-3.98??g/ml. A subsequent in vitro investigation against the bacterial DNA gyrase target enzyme revealed a significant potent inhibitory activity of quinoline derivative 14, which can be observed from its IC50 value (3.39??M). Also, a molecular docking study of the most active compounds was carried out to explore the binding affinity of the new ligands toward the active site of DNA gyrase enzyme as a proposed target of their activity. Furthermore, the ADMET profiles of the most highly effective derivatives were analyzed to evaluate their potentials to be developed as good drug candidates. © 2020 Deutsche Pharmazeutische Gesellschaft. El-Shershaby Mohamed H MH Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt. El-Gamal Kamal M KM Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt. Bayoumi Ashraf H AH Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt. El-Adl Khaled K http://orcid.org/0000-0002-8922-9770 Pharmaceutical Medicinal Chemistry & Drug Design Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Heliopolis University for Sustainable Development, Cairo, Egypt. Ahmed Hany E A HEA http://orcid.org/0000-0001-8898-8452 Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt. Pharmacognosy and Pharmaceutical Chemistry Department, Taibah University, Al-Madinah Al-Munawarah, Saudi Arabia. Abulkhair Hamada S HS http://orcid.org/0000-0001-6479-4573 Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Horus University, New Damietta, Egypt. eng Journal Article 2020 10 20 Germany Arch Pharm (Weinheim) 0330167 0365-6233 IM DNA gyrase antimicrobial molecular docking quinoline synthesis 2020 07 29 2020 09 17 2020 09 23 2020 10 20 8 38 2020 10 21 6 0 2020 10 21 6 0 aheadofprint 33078877 10.1002/ardp.202000277 REFERENCES, 2020</i></font><br><font color=#008000>http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0<br></font></span><br>92.  <a href=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0 class=title>LINC01133 promotes the progression of cervical cancer via regulating miR-30a-5p/FOXD1.</a><a href=http://ubio.org/tools/linkit.php?map%5B%5D=all&link_type=2&url=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0><img src=linkit.png border=0 title='LinkIT' alt='LinkIT'></a> <br><span class=j>Zhang D, Zhang Y, Sun X<br><font color=gray><i>Asia-Pacific journal of clinical oncology Asia Pac J Clin Oncol LINC01133 promotes the progression of cervical cancer via regulating miR-30a-5p/FOXD1. 10.1111/ajco.13451 The prognosis of patients with recurrent or metastatic cervical cancer (CC) remains poor, and its incidence is especially high in developing countries. Multiple long noncoding RNAs are recently identified as crucial oncogenic factors or tumor suppressors. In this study, we explored the function and mechanism of LINC01133 during the progression of CC. Expression levels of LINC01133 and miR-30a-5p in 50 CC tissue samples were measured using quantitative real-time polymerase chain reaction. Immunohistochemistry and Western blot analysis were used to detect the expression of oncogene forkhead box D1 (FOXD1). The association between pathological indices and the expression level of LINC01133 was also analyzed. Human CC cell lines HeLa and SiHa were used as cell models. CCK-8 and bromodeoxyuridine assays were used to assess the effect of LINC01133 on CC cell line proliferation. Flow cytometry was used to study the effect of LINC01133 on CC apoptosis. Transwell assay was conducted to detect the effect of LINC01133 on migration and invasion. Furthermore, luciferase reporter assay was used to confirm the targeting relationship between miR-30a-5p to LINC01133. We observed that LINC01133 expression in CC clinical samples was significantly increased, with high expression associated with higher T stage and negative HPV infection of the patients. Its overexpression remarkably accelerated proliferation and metastasis of CC cells, with reduced apoptosis. LINC01133 knockdown suppressed the malignant phenotypes of CC cells. Overexpression of LINC01133 significantly reduced the expression of miR-30a-5p by sponging it and enhanced the expression of FOXD1. We report the overexpression of LINC01133 in CC sample and cell lines, which correlated with unfavorable pathological indices. LINC01133 was a sponge of tumor suppressor miR-30a-5p, and it enhanced the expression of FOXD1 indirectly and functioned as an oncogenic lncRNA in CC. © 2020 John Wiley & Sons Australia, Ltd. Zhang Dan D Department of Gynecology, General Hospital of Fushun Mining Bureau of Liaoning Health Industry Group, Fushun, Liaoning Province, China. Zhang Yuyang Y https://orcid.org/0000-0003-3566-4037 The Second Department of Oncology, General Hospital of Fushun Mining Bureau of Liaoning Health Industry Group, Fushun, Liaoning Province, China. Sun Xiuyun X Department of Gynecology, General Hospital of Fushun Mining Bureau of Liaoning Health Industry Group, Fushun, Liaoning Province, China. eng Natural Science Foundation of Liaoning Province Journal Article 2020 10 20 Australia Asia Pac J Clin Oncol 101241430 1743-7555 IM FOXD1 LINC01133 cervical cancer miR-30a-5p 2019 09 04 2020 07 12 2020 07 30 2020 10 20 8 39 2020 10 21 6 0 2020 10 21 6 0 aheadofprint 33078907 10.1111/ajco.13451 REFERENCES, 2020</i></font><br><font color=#008000>http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0<br></font></span><br>93.  <a href=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0 class=title>Prognostic performance of qSOFA in oncology patients admitted to the emergency department with suspected infection.</a><a href=http://ubio.org/tools/linkit.php?map%5B%5D=all&link_type=2&url=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0><img src=linkit.png border=0 title='LinkIT' alt='LinkIT'></a> <br><span class=j>Koh TL, Canet E, Amjad S, Bellomo R, Taylor D, Gan HK, Marhoon N, Lim A, Ong WL, Krishnan V, Khor R<br><font color=gray><i>Asia-Pacific journal of clinical oncology Asia Pac J Clin Oncol Prognostic performance of qSOFA in oncology patients admitted to the emergency department with suspected infection. 10.1111/ajco.13422 We aimed to test the performance of the quick Sequential Organ Failure Assessment score (qSOFA) in predicting the outcomes of oncology patients admitted to the emergency department (ED) with suspected infection. Retrospective cohort analysis of all oncology patients presenting to the ED of a tertiary hospital with suspected infection from 1 December 2014 to 1 June 2017. Patients were identified by cross-linkage of ED and Oncology electronic health records. The primary outcome was in-hospital mortality and/or ICU stay ? 3 days. A total of 1655 patients were included in this study--1267 (76.6%) with solid tumor and 388 (23.4%) with hematological malignancies. At presentation, 495 patients had chemotherapy, and 140 had radiotherapy within the preceding 6 months. Four hundred patients received chemotherapy and/or radiotherapy in the previous 4 weeks. Overall, 371 (22.4%) patients had qSOFA ? 2. Such patients had a higher likelihood of respiratory infections compared to patients with a qSOFA < 2 (43.9% vs 29%) and were more likely to be admitted to ICU or require mechanical ventilation. In-hospital mortality or in-hospital mortality and/or ICU stay ? 3 days were 17.3% and 21%, for qSOFA ? 2 patients versus 4.7% and 6.9% for qSOFA < 2 patients (P < .001). qSOFA ? 2 had a negative predictive value of 95% for in-hospital mortality and 93% for in-hospital mortality or ICU stay ? 3 days. Among oncology patients presenting to the ED with suspected infection, a qSOFA ? 2 is associated with a threefold risk of hospital mortality/prolonged ICU stay. Its absence helps identify low-risk patients. © 2020 John Wiley & Sons Australia, Ltd. Koh Tze Lui TL https://orcid.org/0000-0001-6828-6445 Department of Radiation Oncology, Olivia Newton-John Cancer Wellness and Research Centre, Austin Health, Heidelberg, Victoria, Australia. Canet Emmanuel E Medical ICU, Hôtel-Dieu, University Hospital, Nantes, Loire-Atlantique, France. Amjad Sobia S University of Melbourne, Parkville, Victoria, Australia. Bellomo Rinaldo R ICU, Austin Health, Heidelberg, Victoria, Australia. Taylor David D University of Melbourne, Parkville, Victoria, Australia. Emergency Department, Austin Health, Heidelberg, Victoria, Australia. Gan Hui K HK Medical Oncology, Olivia Newton-John Cancer Wellness and Research Centre, Austin Health, Heidelberg, Victoria, Australia. La Trobe University School of Cancer Medicine, Heidelberg, Victoria, Australia. Department of Medicine, University of Melbourne, Heidelberg, Victoria, Australia. Marhoon Nada N Medical Oncology, Olivia Newton-John Cancer Wellness and Research Centre, Austin Health, Heidelberg, Victoria, Australia. Lim Andrew A Medical Oncology, Olivia Newton-John Cancer Wellness and Research Centre, Austin Health, Heidelberg, Victoria, Australia. Ong Wee Loon WL https://orcid.org/0000-0001-6657-7193 Department of Radiation Oncology, Olivia Newton-John Cancer Wellness and Research Centre, Austin Health, Heidelberg, Victoria, Australia. Department of Epidemiology and Preventive Medicine, Monash University, Melbourne, Victoria, Australia. Health and Biomedical Informatics Centre, University of Melbourne, Melbourne, Victoria, Australia. School of Clinical Medicine, University of Cambridge, Cambridge, UK. Krishnan Vivek V MKM Health, South Yarra, Victoria, Australia. Khor Richard R Department of Radiation Oncology, Olivia Newton-John Cancer Wellness and Research Centre, Austin Health, Heidelberg, Victoria, Australia. eng Journal Article 2020 10 20 Australia Asia Pac J Clin Oncol 101241430 1743-7555 IM cancer chemotherapy qSOFA radiotherapy sepsis septic shock 2020 01 17 2020 06 07 2020 06 16 2020 10 20 8 38 2020 10 21 6 0 2020 10 21 6 0 aheadofprint 33078888 10.1111/ajco.13422 REFERENCES, 2020</i></font><br><font color=#008000>http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0<br></font></span><br>94.  <a href=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0 class=title>Reaction of Cu(II) Chelates with Uranyl Nitrate to Form a Coordination Complex or H-Bonded Adduct: Experimental Observations and Rationalization by Theoretical Calculations.</a><a href=http://ubio.org/tools/linkit.php?map%5B%5D=all&link_type=2&url=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0><img src=linkit.png border=0 title='LinkIT' alt='LinkIT'></a> <br><span class=j>Bhunia P, Ghosh S, Gomila RM, Frontera A, Ghosh A<br><font color=gray><i>Inorganic chemistry, 2020</i></font><br><font color=#008000>http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0<br></font></span><br>95.  <a href=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0 class=title>Primary Treatment Selection for Clinically Node-<b>Negative</b> Merkel Cell Carcinoma of the Head and Neck.</a><a href=http://ubio.org/tools/linkit.php?map%5B%5D=all&link_type=2&url=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0><img src=linkit.png border=0 title='LinkIT' alt='LinkIT'></a> <br><span class=j>Jacobs D, Olino K, Park HS, Clune J, Cheraghlou S, Girardi M, Burtness B, Kluger H, Judson BL<br><font color=gray><i>Otolaryngology--head and neck surgery : official journal of American Academy of Otolaryngology-Head and Neck Surgery, 2020</i></font><br><font color=#008000>http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0<br></font></span><br>96.  <a href=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0 class=title>First Report of Garlic virus B infecting Garlic in India.</a><a href=http://ubio.org/tools/linkit.php?map%5B%5D=all&link_type=2&url=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0><img src=linkit.png border=0 title='LinkIT' alt='LinkIT'></a> <br><span class=j>Roylawar PB, Khandagale KS, Randive P, Atre GE, Gawande SJ, Singh M<br><font color=gray><i>Plant disease, 2020</i></font><br><font color=#008000>http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0<br></font></span><br>97.  <a href=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0 class=title>Reducing Chlorothalonil Use in Fungicide Spray Programs for Powdery Mildew, Anthracnose, and Gummy Stem Blight in Melons.</a><a href=http://ubio.org/tools/linkit.php?map%5B%5D=all&link_type=2&url=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0><img src=linkit.png border=0 title='LinkIT' alt='LinkIT'></a> <br><span class=j>Jones JG, Korir RC, Walter TL, Everts KL<br><font color=gray><i>Plant disease, 2020</i></font><br><font color=#008000>http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0<br></font></span><br>98.  <a href=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0 class=title>Intra-articular Corticosteroid Injections for the Treatment of Hip and Knee Osteoarthritis-related Pain: Considerations and Controversies with a Focus on Imaging-<i>Radiology</i> Scientific Expert Panel.</a><a href=http://ubio.org/tools/linkit.php?map%5B%5D=all&link_type=2&url=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0><img src=linkit.png border=0 title='LinkIT' alt='LinkIT'></a> <br><span class=j>Guermazi A, Neogi T, Katz JN, Kwoh CK, Conaghan PG, Felson DT, Roemer FW<br><font color=gray><i>Radiology, 2020</i></font><br><font color=#008000>http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0<br></font></span><br>99.  <a href=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0 class=title>Regulatory Focus and Substance Use in Adolescents: Protective Effects of Prevention Orientation.</a><a href=http://ubio.org/tools/linkit.php?map%5B%5D=all&link_type=2&url=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0><img src=linkit.png border=0 title='LinkIT' alt='LinkIT'></a> <br><span class=j>Franzese AT, Blalock DV, Blalock KM, Wilson SM, Medenblik A, Costanzo PR, Strauman TJ<br><font color=gray><i>Substance use & misuse, 2020</i></font><br><font color=#008000>http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0<br></font></span><br>100.  <a href=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0 class=title>Aborted myocardial infarction in patients with STEMI treated with mechanical reperfusion.</a><a href=http://ubio.org/tools/linkit.php?map%5B%5D=all&link_type=2&url=http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0><img src=linkit.png border=0 title='LinkIT' alt='LinkIT'></a> <br><span class=j>Konarski ?, D?bi?ski M, Kolarczyk-Haczyk A, Jelonek M, Kondys M, Buszman P<br><font color=gray><i>Kardiologia polska, 2020</i></font><br><font color=#008000>http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=0<br></font></span><br><br><br><table cellspacing=0 cellpadding=0 align=center><tr valign=bottom><td align=center><a href=http://ubio.org/portal/index.php?search=negative&category=l&client=pubmed&startPage=9><img src=p.png border=0></a></td><td align=center><a href=http://ubio.org/portal/index.php?search=negative&category=l&client=pubmed&startPage=1><img src=o_yellow.png border=0></a></td><td align=center><a href=http://ubio.org/portal/index.php?search=negative&category=l&client=pubmed&startPage=2><img src=o_yellow.png border=0></a></td><td align=center><a href=http://ubio.org/portal/index.php?search=negative&category=l&client=pubmed&startPage=3><img src=o_yellow.png border=0></a></td><td align=center><a 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