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      Facile and Chemically Sustainable One-Pot Synthesis of a Wide Array of FusedO- andN-Heterocycles Catalyzed by Trisodium Citrate Dihydrate under Ambient Conditions

      1 , 1
      Asian Journal of Organic Chemistry
      Wiley

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          Pyrrolidinyl-spirooxindole natural products as inspirations for the development of potential therapeutic agents.

          The 3,3'-pyrrolidinyl-spirooxindole unit is a privileged heterocyclic motif that forms the core of a large family of alkaloid natural products with strong bioactivity profiles and interesting structural properties. Significant recent advances in the synthesis of this fused heterocyclic system have led to intense interest in the development of related compounds as potential medicinal agents or biological probes.
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            Spiroindolones, a potent compound class for the treatment of malaria.

            Recent reports of increased tolerance to artemisinin derivatives--the most recently adopted class of antimalarials--have prompted a need for new treatments. The spirotetrahydro-beta-carbolines, or spiroindolones, are potent drugs that kill the blood stages of Plasmodium falciparum and Plasmodium vivax clinical isolates at low nanomolar concentration. Spiroindolones rapidly inhibit protein synthesis in P. falciparum, an effect that is ablated in parasites bearing nonsynonymous mutations in the gene encoding the P-type cation-transporter ATPase4 (PfATP4). The optimized spiroindolone NITD609 shows pharmacokinetic properties compatible with once-daily oral dosing and has single-dose efficacy in a rodent malaria model.
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              Structure-based discovery of an organic compound that binds Bcl-2 protein and induces apoptosis of tumor cells.

              Bcl-2 and related proteins are key regulators of apoptosis or programmed cell death implicated in human disease including cancer. We recently showed that cell-permeable Bcl-2 binding peptides could induce apoptosis of human myeloid leukemia in vitro and suppress its growth in severe combined immunodeficient mice. Here we report the discovery of HA14-1, a small molecule (molecular weight = 409) and nonpeptidic ligand of a Bcl-2 surface pocket, by using a computer screening strategy based on the predicted structure of Bcl-2 protein. In vitro binding studies demonstrated the interaction of HA14-1 with this Bcl-2 surface pocket that is essential for Bcl-2 biological function. HA14-1 effectively induced apoptosis of human acute myeloid leukemia (HL-60) cells overexpressing Bcl-2 protein that was associated with the decrease in mitochondrial membrane potential and activation of caspase-9 followed by caspase-3. Cytokine response modifier A, a potent inhibitor of Fas-mediated apoptosis, did not block apoptosis induced by HA14-1. Whereas HA14-1 strongly induced the death of NIH 3T3 (Apaf-1(+/+)) cells, it had little apoptotic effect on Apaf-1-deficient (Apaf-1(-/-)) mouse embryonic fibroblast cells. These data are consistent with a mechanism by which HA14-1 induces the activation of Apaf-1 and caspases, possibly by binding to Bcl-2 protein and inhibiting its function. The discovery of this cell-permeable molecule provides a chemical probe to study Bcl-2-regulated apoptotic pathways in vivo and could lead to the development of new therapeutic agents.
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                Author and article information

                Journal
                Asian Journal of Organic Chemistry
                Asian J. Org. Chem.
                Wiley
                21935807
                February 2016
                February 2016
                January 12 2016
                : 5
                : 2
                : 271-286
                Affiliations
                [1 ]Laboratory of Natural Products & Organic Synthesis; Department of Chemistry; Visva-Bharati (a Central University); Santiniketan 731235 West Bengal India
                Article
                10.1002/ajoc.201500465
                01dc13db-d5ec-46d8-9ee6-8532db58cc75
                © 2016

                http://doi.wiley.com/10.1002/tdm_license_1.1

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