Author
Surya K. De
Other affiliations: National Dairy Research Institute, University of Calcutta, University of Washington ...read more
Bio: Surya K. De is an academic researcher from University of California, Riverside. The author has contributed to research in topics: Trifluoromethanesulfonate & Catalysis. The author has an hindex of 29, co-authored 140 publications receiving 3133 citations. Previous affiliations of Surya K. De include National Dairy Research Institute & University of Calcutta.
Papers published on a yearly basis
Papers
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TL;DR: In this article, substituted benzimidazoles have been synthesized in a single pot under solvent-free conditions from o -phenylenediamine and aldehydes in the presence of a catalytic amount of In(OTf) 3 at room temperature.
Abstract: 2-Substituted benzimidazoles have been synthesized in excellent yields in a single pot under solvent-free conditions from o -phenylenediamine and aldehydes in the presence of a catalytic amount of In(OTf) 3 at room temperature.
180 citations
TL;DR: A series of small molecules JIP1 mimics that function as substrate competitive inhibitors of JNK are reported, one of which, BI-78D3, dose-dependently inhibits the phosphorylation of J NK substrates both in vitro and in cell.
Abstract: JNK is a stress-activated protein kinase that modulates pathways implicated in a variety of disease states. JNK-interacting protein-1 (JIP1) is a scaffolding protein that enhances JNK signaling by creating a proximity effect between JNK and upstream kinases. A minimal peptide region derived from JIP1 is able to inhibit JNK activity both in vitro and in cell. We report here a series of small molecules JIP1 mimics that function as substrate competitive inhibitors of JNK. One such compound, BI-78D3, dose-dependently inhibits the phosphorylation of JNK substrates both in vitro and in cell. In animal studies, BI-78D3 not only blocks JNK dependent Con A-induced liver damage but also restores insulin sensitivity in mouse models of type 2 diabetes. Our findings open the way for the development of protein kinase inhibitors targeting substrate specific docking sites, rather than the highly conserved ATP binding sites. In view of its favorable inhibition profile, selectivity, and ability to function in the cellular milieu and in vivo, BI-78D3 represents not only a JNK inhibitor, but also a promising stepping stone toward the development of an innovative class of therapeutics.
179 citations
TL;DR: In this article, a straightforward and general method was developed for the synthesis of polyhydroquinolines derivatives by simply combining aldehyde, ethyl acetoacetate, dimedone, and ammonium acetate in the presence of a catalytic amount of scandium triflate.
Abstract: A straightforward and general method has been developed for the synthesis of polyhydroquinolines derivatives by simply combining aldehyde, ethyl acetoacetate, dimedone, and ammonium acetate in the presence of a catalytic amount of scandium triflate. This method is very easy, rapid, and high yielding reaction for the synthesis of polyhydroquinolines.
150 citations
TL;DR: In this article, 2-Aminoaryl ketones undergo condensation with α-methylene ketones in the presence of a catalytic amount of Y(OTf)3 at room temperature under mild conditions to afford the corresponding polysubstituted quinolines in excellent yields.
135 citations
TL;DR: A simple and efficient one-pot method for α-aminonitriles from aldehydes, amines, and trimethylsilyl cyanide in the presence of a catalytic amount of bismuth trichloride was developed in this paper.
125 citations
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TL;DR: This Review highlights the recent progress made in defining the functions of the JNK and p38 MAPK pathways in different cancers.
Abstract: Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase (MAPK) family members function in a cell context-specific and cell type-specific manner to integrate signals that affect proliferation, differentiation, survival and migration. Consistent with the importance of these events in tumorigenesis, JNK and p38 MAPK signalling is associated with cancers in humans and mice. Studies in mouse models have been essential to better understand how these MAPKs control cancer development, and these models are expected to provide new strategies for the design of improved therapeutic approaches. In this Review we highlight the recent progress made in defining the functions of the JNK and p38 MAPK pathways in different cancers.
2,164 citations
TL;DR: One of the goals of this Review is to attract the attention of the scientific community as to the benefits of using hypervalent iodine compounds as an environmentally sustainable alternative to heavy metals.
Abstract: The preparation, structure, and chemistry of hypervalent iodine compounds are reviewed with emphasis on their synthetic application. Compounds of iodine possess reactivity similar to that of transition metals, but have the advantage of environmental sustainability and efficient utilization of natural resources. These compounds are widely used in organic synthesis as selective oxidants and environmentally friendly reagents. Synthetic uses of hypervalent iodine reagents in halogenation reactions, various oxidations, rearrangements, aminations, C–C bond-forming reactions, and transition metal-catalyzed reactions are summarized and discussed. Recent discovery of hypervalent catalytic systems and recyclable reagents, and the development of new enantioselective reactions using chiral hypervalent iodine compounds represent a particularly important achievement in the field of hypervalent iodine chemistry. One of the goals of this Review is to attract the attention of the scientific community as to the benefits of...
1,228 citations
TL;DR: A deep neural network capable of predicting molecules with antibacterial activity is trained and a molecule from the Drug Repurposing Hub-halicin- is discovered that is structurally divergent from conventional antibiotics and displays bactericidal activity against a wide phylogenetic spectrum of pathogens.
1,002 citations
TL;DR: The ability of proline to influence disparate cellular outcomes may be governed by ROS levels generated in the mitochondria, and defining the threshold at which proline metabolic enzyme expression switches from inducing survival pathways to cellular apoptosis would provide molecular insights into cellular redox regulation by proline.
Abstract: Significance: The imino acid proline is utilized by different organisms to offset cellular imbalances caused by environmental stress. The wide use in nature of proline as a stress adaptor molecule indicates that proline has a fundamental biological role in stress response. Understanding the mechanisms by which proline enhances abiotic/biotic stress response will facilitate agricultural crop research and improve human health. Recent Advances: It is now recognized that proline metabolism propels cellular signaling processes that promote cellular apoptosis or survival. Studies have shown that proline metabolism influences signaling pathways by increasing reactive oxygen species (ROS) formation in the mitochondria via the electron transport chain. Enhanced ROS production due to proline metabolism has been implicated in the hypersensitive response in plants, lifespan extension in worms, and apoptosis, tumor suppression, and cell survival in animals. Critical Issues: The ability of proline to influence...
746 citations
TL;DR: This review evaluates the dynamic interactions of cancer cells with their microenvironment consisting of stromal cells and extracellular matrix components in various advanced cancer models, with a focus on 3D systems as well as lab-on-chip devices.
Abstract: The dynamic interactions of cancer cells with their microenvironment consisting of stromal cells (cellular part) and extracellular matrix (ECM) components (non-cellular) is essential to stimulate the heterogeneity of cancer cell, clonal evolution and to increase the multidrug resistance ending in cancer cell progression and metastasis. The reciprocal cell-cell/ECM interaction and tumor cell hijacking of non-malignant cells force stromal cells to lose their function and acquire new phenotypes that promote development and invasion of tumor cells. Understanding the underlying cellular and molecular mechanisms governing these interactions can be used as a novel strategy to indirectly disrupt cancer cell interplay and contribute to the development of efficient and safe therapeutic strategies to fight cancer. Furthermore, the tumor-derived circulating materials can also be used as cancer diagnostic tools to precisely predict and monitor the outcome of therapy. This review evaluates such potentials in various advanced cancer models, with a focus on 3D systems as well as lab-on-chip devices.
693 citations