Browsing by Author "Kaur, G."

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Anticancer activity of dihydropyrazolo[1,5-c]quinazolines against rat C6 glioma cells via inhibition of topoisomerase II
(Wiley-VCH Verlag, 2018) Kaur, G.; Cholia, R.P.; Joshi, G.; Amrutkar, S.M.; Kalra, S.; Mantha, Anil K.; Banerjee, U.C.; Kumar, Raj
The design and synthesis of dihydropyrazolo[1,5-c]quinazolines (1a?h) as human topoisomerase II (TopoII) catalytic inhibitors are reported. The compounds were investigated for their antiproliferative activity against the C6 rat glial cell line. Two compounds, 1b and 1h, were found to be potent cytotoxic agents against glioma cells and exerted selective TopoII inhibitory activity. Furthermore, the compounds induced alterations in reactive oxygen species levels as measured by DCFDA assay and were found to induce cell cycle arrest at the G1 phase at lower concentrations and profound apoptosis at higher concentrations. The interaction of selected investigational molecules with TopoII was further corroborated by molecular modeling. ? 2018 Deutsche Pharmazeutische Gesellschaft
Effects of Environmental Pesticides on the Health of Rural Communities in the Malwa Region of Punjab, India: A Review
(2014) Mittal, S.; Kaur, G.; Vishwakarma, G.S.
The Malwa region of Punjab, India, is facing an unprecedented crisis of environmental health linked to indiscriminate, excessive, and unsafe use of pesticides, fertilizers, and poor groundwater quality. The region has been described as India's "cancer capital" due to abnormally high number of cancer cases, which have increased 3-fold in the last 10 years. Studies of this region have also highlighted a sharp increase in many other pesticide-related diseases, such as mental retardation and reproductive disorders. The most affected individuals are the agricultural workers who are directly exposed to pesticides. The Malwa region of Punjab, India, is less than 15% of the total area of Punjab (only 0.5% of the total geographical area of India), but it consumes nearly 75% of the total pesticides used in Punjab. The high use of pesticides, along with environmental and social factors, is responsible for the high concentration of pesticide residues in the food chain of this region. Moreover, many banned and restricted pesticides are still in use in this region, warranting strict periodical health checkups and other interventions. The present review describes occupational, environmental, and social factors associated with pesticide use in the Malwa region of Punjab, India, and proposes some risk reduction interventions. ? 2014 Copyright Taylor and Francis Group, LLC.
Interaction between topoisomerases and histone deacetylases: Role in cancer progression and therapeutic interventions
(Nova Science Publishers, Inc., 2017) Joshi, G.; Thakur, A.; Kaur, G.; Kalra, S.; Singh, S.; Kumar, R.
DNA topoisomerases are termed as the magicians of the DNA world, as they are involved in overcoming all the topological DNA problems. Histone Deacetylases are the collection of enzymes that assist in the regulation of DNA control. The overexpression of topoisomerases and histone deacetylases are found in various diseases including cancer. Till date, many therapies have been discovered to target topoisomerases and histone deacetylases individually. However, most of these treatments are associated with the toxicities and drug resistance. The drug resistance apart from known mechanism(s) could occur due to crosstalk(s) of topoisomerases with various proteins associated directly or indirectly with the cancer prognosis. Histone deacetylases that render topoisomerase inhibitors resistant also insensitize them toward binding to the receptor. The chapter overlays the discussion on the underlying mechanism(s) involved in topoisomerase and histone deacetylases interactions. The chapter also congregates the information suggested for the essential pharmacophore development for such hybrid drug discovery. The attempt has also been made to give a preliminary virtual background on the fundamental interaction of these two proteins along with the primary amino acids involved in such interaction. ? 2017 Nova Science Publishers, Inc.