Pharmaceutical Sciences and Natural Products - Research Publications
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Item Seven-membered ring fused pyrimidine-based derivatives and their biological properties(Elsevier, 2022-10-14T00:00:00) Kaur, Manpreet; Kumar, RajIn the chapter, the synthesis along-with the biological importance of seven-membered ring fused pyrimidine-based derivatives has been discussed, where the seven-membered rings may consist of heteroatoms such as sulfur, oxygen, and nitrogen, which are supposed to provide important binding interactions within the binding pocket of certain receptors/enzymes like Epidermal growth factor receptor, HER, etc. � 2023 Elsevier Ltd. All rights reserved.Item A Minireview on the Scope of Cadogan Cyclization Reactions Leading to Diverse Azaheterocycles(John Wiley and Sons Inc, 2022-04-01T00:00:00) Kaur, Manpreet; Kumar, RajFrom the last two decades, Cadogan cyclization reaction is considered as one of the best routes for the preparation of various azaheterocycles comprising carbazoles, indoles, coumarins, carbolines, pyrazoloquinoxalines, S,N-heterotetracenes from the nitro-based substrates by using a variety of tetravalent phosphorus-based reagents. To date the majority of Cadogan reactions are found to be intramolecular reactions, however, interestingly, a case of intermolecular Cadogan reaction is also reported, resulting in the widening of the reaction scope for futuristic perspectives. We report the Cadogan cyclization reactions for the synthesis of azaheterocycles from 2018 to present according to multiple classes of chemical frameworks including its scope (FDA approved drugs), along with the possibilities and mechanistic developments for unexpected products. � 2022 Wiley-VCH GmbH.Item Synthesis of 1,4-dihydropyrazolo[4,3-b]indoles via intramolecular C(sp2)-N bond formation involving nitrene insertion, DFT study and their anticancer assessment(Academic Press Inc., 2021-06-29T00:00:00) Kaur, Manpreet; Mehta, Vikrant; Abdullah Wani, Aabid; Arora, Sahil; Bharatam, Prasad V.; Sharon, Ashoke; Singh, Sandeep; Kumar, RajWe herein report a new synthetic route for a series of unreported 1,4-dihydropyrazolo[4,3-b]indoles (6�8) via deoxygenation of o-nitrophenyl-substituted N-aryl pyrazoles and subsequent intramolecular (sp2)-N bond formation under microwave irradiation expedite modified Cadogan condition. This method allows access to NH-free as well as N-substituted fused indoles. DFT study and controlled experiments highlighted the role of nitrene insertion as one of the plausible reaction mechanisms. Furthermore, the target compounds exhibited cytotoxicity at low micromolar concentration against lung (A549), colon (HCT-116), and breast (MDA-MB-231, and MCF-7) cancer cell lines, induced the ROS generation and altered the mitochondrial membrane potential of highly aggressive MDA-MB-231 cells. Further investigations revealed that these compounds were selective Topo I (6h) or Topo II (7a, 7b) inhibitors. � 2021 Elsevier Inc.Item Dynamic Axial Chirality in Drug Design and Discovery: Introduction to Atropisomerism, Classification, Significance, Recent Trends and Challenges(Springer Singapore, 2021-02-18T00:00:00) Joshi, Gaurav; Kaur, Manpreet; Kumar, RajInduction of chirality in non-chiral ligands via involvement of hindered rotation around a single bond has led to the development of atropisomers. The atropisomers behave similarly as the chiral compounds and impact the drug discovery process. The chapter deals importantly with the brief introduction to this class, nomenclature descriptors, methods to measure atropisomers racemization, and the impact of atropisomers on drug discovery and includes relevant examples of drugs both from synthetic and natural origin. The chapter further extends to deal with various methodologies involved in atropselective conversions and regulatory guidelines involved in the development of atropisomers. � Springer Nature Singapore Pte Ltd. 2021.Item C‐N and N‐N bond formation via Reductive Cyclization: Progress in Cadogan /Cadogan‐Sundberg Reaction.(wiley, 2018) Kaur, Manpreet; Kumar, Raj KumarCadogan/Cadogan‐Sundberg cyclization reaction has been reported as one of the most efficient routes for the synthesis of a wide variety of N‐heterocycles from the easily accessible starting materials such as o‐nitrobiaryls or o‐nitroarenes, o‐nitrostyrenes by treating with tetravalent phosphorus compounds (trialkyl or triaryl phosphines or trialkyl phosphites). The reaction has been successfully employed in Carbon‐Carbon as well as Carbon‐Nitrogen bond formation for the scaffolds like carbazole, indoles, coumarins, and indazoles. To the best of authors’ knowledge, the present review is the first compilation of the literature from almost two decades (2000 to present) on Cadogan/Cadogan‐Sundberg cyclization reaction, its scope, mechanistic aspects, and limitations.Item Toward an Understanding of Structural Insights of Xanthine and Aldehyde Oxidases: An Overview of their Inhibitors and Role in Various Diseases(John Wiley and Sons Inc., 2018) Kumar, Raj; Joshi, Gaurav; Kler, Harveen; Kalra, Sourav; Kaur, Manpreet; Arya, RamandeepAlmost all drug molecules become the substrates for oxidoreductase enzymes, get metabolized into more hydrophilic products and eliminated from the body. These metabolites sometime may be more potent, active, inactive, or toxic in nature compared to parent molecule. Xanthine oxidoreductase and aldehyde oxidase belong to molybdenum containing family and are well characterized for their structures and functions, in particular to their ability to oxidize/hydroxylate the xenobiotics. Their upregulated clinical levels causing oxidative stress are associated with pathways either directly involved in the progression of diseases, gout, or indirectly with the succession of other diseases such as diabetes, cancer, etc. Herein, we have put forth a comprehensive review on the xanthine and aldehyde oxidases pertaining to their structures, functions, pathophysiological role, and a comparative analysis of structural insights of xanthine and aldehyde oxidases? binding domains with endogenous ligands or inhibitors. Though both the enzymes are molybdenum containing and are likely to share some common pathways and interact with inhibitors in a similar manner but we have focused on structural prerequisites for inhibitor specificity to both the enzymes keeping in view of the existing X-ray structures. This review also provides futuristic implications in the design of inhibitors derived from inorganic complexes or small organic molecules considering the spatial features and structural insights of both the enzymes. ? 2017 Wiley Periodicals, Inc.