Synthesis and Leukemia Cell Growth Inhibition of a Series of 1,3-Dithiazolylbenzene Derivatives

2004 ◽  
Vol 69 (7) ◽  
pp. 1491-1498 ◽  
Author(s):  
Irene M. Lagoja ◽  
Koen Nauwelaerts ◽  
Christine Bal-Mahieu ◽  
Michela Pasqualini ◽  
Christian Bailly ◽  
...  
Keyword(s):  
Nmr Spectroscopy ◽  
Antitumor Activity ◽  
Rna Viruses ◽  
Leukemia Cell ◽  
Dna Interaction ◽  
Benzene Derivatives ◽  
Cell Growth Inhibition ◽  
Dna And Rna ◽  
Hiv 1 ◽  
Potential Antitumor

By a slightly modified Hantzsch thiazole synthesis either 1,3-bis[(thiazol-2-yl)amino]benzene derivatives 2 or 1,3-bis[2-iminothiazol-3(2H)-yl]benzene derivatives 3 were exclusively obtained. The compounds can be distinguished by NMR spectroscopy. Compounds 2a-2d and 3a-3d were evaluated for their potential antitumor activity, DNA interaction, and for their activity against DNA and RNA viruses and against HIV-1 and HIV-2.

scholarly journals Varicella (Human Herpes Virus-3) Vaccine Potential Role Against Herpes (HSV-1/HSV-2) Viruses to Prevent HIV-1 Pandemic in Sub- Saharan Africa

2018 ◽  
Vol 10 (1) ◽  
pp. 116-123
Author(s):  
Jacqueline Le Goaster ◽  
Patrice Bourée ◽  
Franck N. El Sissy ◽  
Johanna Pokossy Epee ◽  
Frédéric Tangy ◽  
...  
Keyword(s):  
Immune Deficiency ◽  
Rna Viruses ◽  
Varicella Vaccine ◽  
Sub Saharan Africa ◽  
Dna And Rna ◽  
Aids Pandemic ◽  
Recurrent Herpes ◽  
Sub Saharan ◽  
Hiv 1 ◽  
Hsv 1

Background: Synergy exists between DNA and RNA viruses. It was found that the Human Immunodeficiency Viruses (HIV-1) are RNA viruses at the origin of Acquired Immune Deficiency Syndrome (AIDS). The DNA recurrent herpes diseases are associated to AIDS virus at the origin of Sub-Saharan cancer AIDS pandemic. Objective: It is speculated that a varicella virus (HHV-3) immune defect could originate HSV- 1/HSV-2 recurrent herpes diseases that can be cured by varicella vaccine (2012). Methods: At a Symposium held in Kampala, Uganda (1962), impressive Sub-Saharan cancer epidemics: Hodgkin lymphomas and Kaposi sarcomas have been reported since the onset of the 20th century and remained unexplained. Over one thousand publications related to these cancer epidemics were presented. For millenniums, Bantu populations have been living in tropical forests close to chimpanzees infected by Simian Immune Deficiency viruses (SIV). SIV became Human Immune Deficiency viruses (HIV-1). AIDS is a zoonosis. Results: The DNA and RNA viruses, herpes with HIV-1 viruses, are correlated to Sub- Saharan AIDS infections. They induce an extensive immune deficiency with other herpes viruses such as HHV-4 and HHV-8, which are linked to lymphomas and Kaposi sarcomas. It is postulated that a primary HHV-3 immune weakness could be linked to herpes partnership with AIDS pandemic. Conclusion: The Oka, anti-HHV-3, varicella vaccine is able to cure HSV1/HSV2 recurrent herpes diseases. It induces a specific increase of the varicella antibodies. Thus varicella vaccination could prevent herpes recurrences in Sub-Saharan Africa. One- child dose varicella vaccine could be proposed as the first step to overcome HHV-3 herpes deficiency in order to prevent AIDS pandemic.

Application of a Validated QSTR Model for Repurposing COX-2 Inhibitor Coumarin Derivatives as Potential Antitumor Agents

2019 ◽  
Vol 19 (13) ◽  
pp. 1121-1128 ◽  
Author(s):  
Gulcin Tugcu ◽  
Hande Sipahi ◽  
Ahmet Aydin
Keyword(s):  
Antitumor Activity ◽  
Drug Development ◽  
Linear Model ◽  
Cell Lines ◽  
Cyclooxygenase 2 ◽  
Large Set ◽  
Coumarin Derivatives ◽  
Antitumor Compounds ◽  
Cyclooxygenase 2 Inhibitors ◽  
Potential Antitumor

Background: The discovery of novel potent molecules for both cancer prevention and treatment has been continuing over the past decade. In recent years, identification of new, potent, and safe anticancer agents through drug repurposing has been regarded as an expeditious alternative to traditional drug development. The cyclooxygenase-2 is known to be over-expressed in several types of human cancer. For this reason cyclooxygenase-2 inhibition may be useful tool for cancer chemotherapy. Objective: The first aim of the study was to develop a validated linear model to predict antitumor activity. Subsequently, applicability of the model for repurposing these cyclooxygenase-2 inhibitors as antitumor compounds to abridge drug development process. Method: We performed a quantitative structure-toxicity relationship (QSTR) study on a set of coumarin derivatives using a large set of molecular descriptors. A linear model predicting growth inhibition on leukemia CCRF cell lines was developed and consequently validated internally and externally. Accordingly, the model was applied on a set of 143 cyclooxygenase-2 inhibitor coumarin derivatives to explore their antitumor activity. Results: The results indicated that the developed QSAR model would be useful for estimating inhibitory activity of coumarin derivatives on leukemia cell lines. Electronegativity was found to be a prominent property of the molecules in describing antitumor activity. The applicability domain of the developed model highlighted the potential antitumor compounds. Conclusion: The promising results revealed that applied integrated in silico approach for repurposing by combining both the biological activity similarity and the molecular similarity via the computational method could be efficiently used to screen potential antitumor compounds among cyclooxygenase-2 inhibitors.

scholarly journals Lactoferrin affects rhinovirus B-14 entry into H1-HeLa cells

2021 ◽  
Vol 166 (4) ◽  
pp. 1203-1211
Author(s):  
Caio Bidueira Denani ◽  
Antonio Real-Hohn ◽  
Carlos Alberto Marques de Carvalho ◽  
Andre Marco de Oliveira Gomes ◽  
Rafael Braga Gonçalves
Keyword(s):  
Innate Immune System ◽  
Rna Viruses ◽  
Innate Immune ◽  
Bovine Lactoferrin ◽  
Respiratory Illnesses ◽  
Dna And Rna ◽  
Viral Particles ◽  
The Common ◽  
Additional Influence

AbstractLactoferrin is part of the innate immune system, with antiviral activity against numerous DNA and RNA viruses. Rhinoviruses, the leading cause of the common cold, are associated with exacerbation of respiratory illnesses such as asthma. Here, we explored the effect of bovine lactoferrin (BLf) on RV-B14 infectivity. Using different assays, we show that the effect of BLf is strongest during adhesion of the virus to the cell and entry. Tracking the internalisation of BLf and virus revealed a degree of colocalisation, although their interaction was only confirmed in vitro using empty viral particles, indicating a possible additional influence of BLf on other infection steps.

scholarly journals From Capsids to Complexes: Expanding the Role of TRIM5α in the Restriction of Divergent RNA Viruses and Elements

Viruses ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 446
Author(s):  
Kevin M. Rose ◽  
Stephanie J. Spada ◽  
Rebecca Broeckel ◽  
Kristin L. McNally ◽  
Vanessa M. Hirsch ◽  
...  
Keyword(s):  
Human Immunodeficiency Virus ◽  
Molecular Basis ◽  
Human Population ◽  
Rna Viruses ◽  
Arms Race ◽  
Innate Immune ◽  
Immunodeficiency Virus ◽  
Underlying Mechanisms ◽  
Hiv 1

An evolutionary arms race has been ongoing between retroviruses and their primate hosts for millions of years. Within the last century, a zoonotic transmission introduced the Human Immunodeficiency Virus (HIV-1), a retrovirus, to the human population that has claimed the lives of millions of individuals and is still infecting over a million people every year. To counteract retroviruses such as this, primates including humans have evolved an innate immune sensor for the retroviral capsid lattice known as TRIM5α. Although the molecular basis for its ability to restrict retroviruses is debated, it is currently accepted that TRIM5α forms higher-order assemblies around the incoming retroviral capsid that are not only disruptive for the virus lifecycle, but also trigger the activation of an antiviral state. More recently, it was discovered that TRIM5α restriction is broader than previously thought because it restricts not only the human retroelement LINE-1, but also the tick-borne flaviviruses, an emergent group of RNA viruses that have vastly different strategies for replication compared to retroviruses. This review focuses on the underlying mechanisms of TRIM5α-mediated restriction of retroelements and flaviviruses and how they differ from the more widely known ability of TRIM5α to restrict retroviruses.

scholarly journals Potential Antitumor Activity of SIM-89 in Non-Small Cell Lung Cancer Cells

2017 ◽  
Vol 58 (3) ◽  
pp. 581
Author(s):  
Jun Pei ◽  
Tianqing Chu ◽  
Minhua Shao ◽  
Jiajun Teng ◽  
Huifang Sha ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Antitumor Activity ◽  
Small Cell Lung Cancer ◽  
Cancer Cells ◽  
Cell Lung Cancer ◽  
Small Cell ◽  
Lung Cancer Cells ◽  
Small Cell Lung ◽  
Potential Antitumor
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