Facile Preparation of 1,2-Diketones

Autor: Derek Cecil Cole, Pawel Nowak, David Malwitz

Publikováno v: Synthetic Communications. 40:2164-2171

Easily accessible lead-like libraries of heterocyclic molecules useful for high-throughput screening are of continuous interest to the pharmaceutical industry. A number of drug-like libraries are derived from aromatic 1,2-diketones; however, nonsymme

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b1ef2ae6a70c69d59935744f725f8518
https://doi.org/10.1080/00397910903219575

ATP-Competitive Inhibitors of the Mammalian Target of Rapamycin: Design and Synthesis of Highly Potent and Selective Pyrazolopyrimidines

Autor: David Malwitz, David J. Richard, Kristine Svenson, Lourdes Toral-Barza, Natasja Brooijmans, Ker Yu, Kevin J. Curran, Jeroen C. Verheijen, Judy Lucas, Arie Zask, Pawel Nowak, Joshua Kaplan, Weiguo Zhang, Robert T. Abraham, Irwin Hollander, Joel Bard, James Joseph Gibbons, Semiramis Ayral-Kaloustian, Tarek S. Mansour

Publikováno v: Journal of Medicinal Chemistry. 52:5013-5016

The mammalian target of rapamycin (mTOR), a central regulator of growth, survival, and metabolism, is a validated target for cancer therapy. Rapamycin and its analogues, allosteric inhibitors of mTOR, only partially inhibit one mTOR protein complex.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47c29065dfa8ed03476485767435f485
https://doi.org/10.1021/jm900851f

Discovery of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as highly potent and selective ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR): optimization of the 6-aryl substituent

Autor: Natasja Brooijmans, Ker Yu, Arie Zask, Jeroen C. Verheijen, Judy Lucas, David J. Richard, Semiramis Ayral-Kaloustian, Mark Lefever, Kevin J. Curran, Weiguo Zhang, Lourdes Toral-Barza, Pawel Nowak, Tarek S. Mansour, Irwin Hollander, David Malwitz, Joshua Kaplan

Publikováno v: Journal of medicinal chemistry. 52(24)

Design and synthesis of a series of 4-morpholino-6-aryl-1H-pyrazolo[3,4-d]pyrimidines as potent and selective inhibitors of the mammalian target of rapamycin (mTOR) are described. Optimization of the 6-aryl substituent led to the discovery of inhibit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ec49613908ce202d67c24e3d81a8041
https://pubmed.ncbi.nlm.nih.gov/19894727

Proceedings of the 4th World Conference on Research Integrity

Autor: O’Brien, Susan Patricia, Chan, Danny, Leung, Frederick, Ko, Eun Jung, Kwak, Jin Sun, Gwon, TaeHwan, Lee, Ji Min, Lee, Min-Ho, Nolte, Helga, Gommel, Michael, Sponholz, Gerlinde, Krastev, Yordanka, Sandiran, Yamini, Connell, Julia, Solomon, Nicky, Krasovec, Ursa Opara, Sribar, Renata, Martinson, Brian C., Thrush, Carol R., Gunsalus, C. K., Oransky, Ivan, Marcus, Adam, Graf, Chris, Warne, Verity, Wates, Edward, Joshua, Sue, Roig, Miguel, Mumford, Michael, Deschênes, Mylène, Olivier, Catherine, Dupras-Leduc, Raphaëlle, Hammatt, Zoë, Tamot, Raju, Parker, Robin, Ricard, Cynthia, Nguyen-Khoa, Loc, Titus, Sandra, Jensen, Karsten Klint, Godecharle, Simon, Nemery, Ben, Dierickx, Kris, Gjerris, Mickey, Eriksen, Maud Marion Laird, Hoej, Jeppe Berggren, Steneck, Nicholas H., Nebeker, Camille, Kalichman, Michael, Booen, Elizabeth Mejia, Pacheco, Blanca Azucena, Giacinto, Rebeca Espinosa, Castaneda, Sheila, Li, Ding, Chen, Qiong, Zhu, Guoli, Sun, Zhonghe, Abbasi, Badaruudin, Ganguly, Parthasarathi, Ganguly, Barna, Bonn, Noémie Aubert, Bourcier, Daniele, Bordé, Jacques, Leduc, Michèle, Chou, Chien, Pan, Sophia Jui-An, Tiefenauer, Louis Xaver, Barr, Daniel, Taylor, Paul, Horn, Lyn Margaret, Poff, Deborah, Mavrinac, Martina, Brumini, Gordana, Petrovečki, Mladen, Santos, Christiane Coelho, Vasconcelos, Sonia, Lammey, Rachael, Hartgerink, Chris, van Assen, Marcel, Wicherts, Jelte, Hauge, Hanne Silje, Manka, Aaron, Iturrizaga, Raffael, Foeger, Nicole, Lescano, A. Roxana, Lanata, Claudio, Vasquez, Gissella, Mariana, Leguia, Silva, Marita, Kasper, Mathew, Montero, Claudia, Bausch, Daniel, Lescano, Andres G., Blom, Fenneke, Bouter, Lex, Lategan, Laetus O. K., Manaia, Gustavo Fitas, McCormack, Wayne T., Allen, William L., Connelly, Shane, Crites, Joshua, Engler, Jeffrey, Freedman, Victoria, Garvan, Cynthia W., Haidet, Paul, Hockensmith, Joel, McElroy, William, Sander, Erik, Volpe, Rebecca, Verderame, Michael F., Krstic, Snezana, Handy, Louise, Schaller-Demers, Debra, Lerouge, Inge, Cielen, Gerard, Schoofs, Liliane, Marusic, Ana, Squazzoni, Flaminio, Vaux, David, Al-Wazzan, Khalid, Alorainy, Ibrahim, O’Brien, Nolan, Guerin, Suzanne, Dodd, Philip, Wells, Frank, Blewett, Catherine, Litto, Fredric M., De Lecuona, Itziar, Löfstrom, Erika, Maes, Katrien, Bonn, Noémie, Peatfield, Tony, Boehme, Olivier, Caporale, Cinzia, Fanelli, Daniele, Carfora, John, Strauss, Eric, Lynn, William, De Bruyn, Dieter, Nele, Bracke, De Gelder, Katrien, Van der Burght, Stefanie, e Silva, José Roberto Lapa, Vasconcelos, Sonia M. R., Ingierd, Helene, Frankel, Mark, Vasgird, Daniel, Bird, Stephanie, Yarborough, Mark, Garner, Harold, Campo-Engelstein, Lisa, Master, Zubin, Smith, Elise, Resnik, David, Williams-Jones, Bryn, Malicki, Mario, Utrobicic, Ana, Ioannidis, John P. A., ter Riet, Gerben, Walley, Tom, Bouter, Lex Marius, van der Steen, Jenny, Sorenson, Martha, Prosdocimi, Francisco, Masuda, Hatisaburo, Watanabe, Edson, Pinto, José Carlos, Palácios, Marisa, e Silva, José Lapa, Leta, Jacqueline, Vieyra, Adalberto, Pinto, André, Sant’Ana, Mauricio, Shinkai, Rosemary, Yudin, Boris, Vergès, Etienne, Brun-Wauthier, Anne-Sophie, Vial, Géraldine, Vinther, Torkild, Bähr, Volker, Plemmons, Dena, Davies, Rebecca Lynn, Laube, Katrina, Scheopner, Cynthia, Galland, John, Maisonneuve, Hervé, Decullier, Evelyne, Noble, Brian, Gilis, Anja, Gallacher, David J., Lavrijssen, Tom, David, Malwitz, Dasgupta, Malini, Mols, Hans, Savard, Tony, Mah, Eric, Wager, Elizabeth, Kleinert, Sabine, Kiermer, Veronique, Hufton, Andrew, Clyne, Melanie, Almeida, Renan Moritz, Fontes-Pereira, Aldo, Catelani, Fernanda, Rocha, Karina, Iorns, Elizabeth, Gunn, William, Letellier, Lucienne, Malherbe, Cornelia, Kamata, Takehito, Enebakk, Vidar, Penrod, Lynn, Nørgaard, Thomas, Elverdam, Charlotte, Fassin, Yves, Fekken, Cynthia, Adam, Jamal, Anderson, Melissa S., Buttliere, Brett, Groves, Trish, Shanahan, Daniel, Simera, Iveta, Kirtley, Shona, Villanueva, Eleana, Struthers, Caroline, MacCarthy, Angela, Altman, Douglas, Grebenshchikova, Elena, Greene, Bronwyn, Rohr, Ted, Harriman, Stephanie, Varantola, Krista, Opara, Ursa, Rokne, Jon, Setti, Gianluca, MacPherson, Gordon, Hazelkorn, Ellen, Smith, Carthage, McLaughlin, Robert H., Martins, Tatiana Duque, Tanimoto, Tetsuya, Steneck, Nicholas, Kalleberg, Ragnvald, Hussein, Tajammul, Sun, Ping, Tzeng, Ovid, Zimmerman, Susan, Lescano, Roxana, Heitman, Elizabeth, Nieto, Maria Andrea Rocio del Pilar Contre, Fong, Eric, Wilhite, Al, Motta-Roth, Désirée, Tijdink, Joeri, Smulders, Yvo, Steele, Logan, Watts, Logan, Johnson, James, Williams, Lee, Amini, Sufia, Hooft, Lotty, Kilicoglu, Halil, van Seters, Janneke, Eijsackers, Herman, Voragen, Fons, van der Zijpp, Akke, Brom, Frans, Abbasi, Badaruddin, Almasoud, Naif Nasser, Labuschagne, Adri, Severinsen, Johanne, Engh, Espen, Alani, Daham Ismail, Jusoff, H. J. Kamaruzaman, Gordon, Anita, Harton, Helen C., Rocha, Karina de Albuquerque, de Vasconcelos, Sonia Maria Ramos, Matandika, Limbanazo, Prata, Aline Carolina de Oliveira Machado, Neff, Mark William, Costas, Rodrigo, Larivière, Vincent, Filho, Douglas Leonardo Gomes, Guedes, Diego Oliveira, Keller, Niklas, Feufel, Markus, Offenhauser, Nikolas, Kowalczuk, Maria K., Moylan, Elizabeth C., Speanburg, Katie, Lubomirski, Mariusz, Malwitz, David, Gallacher, David, Gillis, Anja, Marques, Maria Betânia de Freitas, Amâncio, Laressa Lima, Fernandes, Raphaela Dias, Patrocínio, Oliveira, Rech, Cláudia Maria Correia Borges, Sousa, Adriana Nascimento, Garcia, Leila Posenato, Patel, Jigisha, Lada, Farida, Di Capua, Giuseppe, Peppoloni, Silvia, DuBois, James M., Chibnall, John, Van der Wall, Jillon, Tait, Raymond, Holen, Jacob, Johannessen, Adele Flakke, Ellefsen, Torunn, Rech, Claudia, Sousa, Adriana, Beranzoli, Laura, Beirão, Paulo S. L.

Publikováno v: Research Integrity and Peer Review. 1(S1)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=core_ac_uk__::eae0faf03cad3f82cea9663152f0398b