Discovery of Quinazolines as Histamine H4 Receptor Inverse Agonists Using a Scaffold Hopping Approach
Smits, Rogier A, de Esch, Iwan J. P, Zuiderveld, Obbe P, Broeker, Joachim, Sansuk, Kamonchanok, Guaita, Elena, Coruzzi, Gabriella, Adami, Maristella, Haaksma, Eric, Leurs, Rob
Published in Journal of medicinal chemistry (25.12.2008)
Published in Journal of medicinal chemistry (25.12.2008)
Get full text
Journal Article
Pan-KRAS inhibitor disables oncogenic signalling and tumour growth
Kim, Dongsung, Herdeis, Lorenz, Rudolph, Dorothea, Zhao, Yulei, Böttcher, Jark, Vides, Alberto, Ayala-Santos, Carlos I., Pourfarjam, Yasin, Cuevas-Navarro, Antonio, Xue, Jenny Y., Mantoulidis, Andreas, Bröker, Joachim, Wunberg, Tobias, Schaaf, Otmar, Popow, Johannes, Wolkerstorfer, Bernhard, Kropatsch, Katrin Gabriele, Qu, Rui, de Stanchina, Elisa, Sang, Ben, Li, Chuanchuan, McConnell, Darryl B., Kraut, Norbert, Lito, Piro
Published in Nature (London) (06.07.2023)
Published in Nature (London) (06.07.2023)
Get full text
Journal Article
Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor
Bröker, Joachim, Waterson, Alex G., Smethurst, Chris, Kessler, Dirk, Böttcher, Jark, Mayer, Moriz, Gmaschitz, Gerhard, Phan, Jason, Little, Andrew, Abbott, Jason R., Sun, Qi, Gmachl, Michael, Rudolph, Dorothea, Arnhof, Heribert, Rumpel, Klaus, Savarese, Fabio, Gerstberger, Thomas, Mischerikow, Nikolai, Treu, Matthias, Herdeis, Lorenz, Wunberg, Tobias, Gollner, Andreas, Weinstabl, Harald, Mantoulidis, Andreas, Krämer, Oliver, McConnell, Darryl B., W. Fesik, Stephen
Published in Journal of medicinal chemistry (10.11.2022)
Published in Journal of medicinal chemistry (10.11.2022)
Get full text
Journal Article
Abstract 1271: In vitro and in vivo characterization of BI 1823911 - a novel KRASG12C selective small molecule inhibitor
Savarese, Fabio, Gollner, Andreas, Rudolph, Dorothea, Lipp, Jesse, Popow, Johannes, Hofmann, Marco H., Arnhof, Heribert, Rinnenthal, Jörg, Trapani, Francesca, Gmachl, Michael, Gerlach, Daniel, Broeker, Joachim, Ettmayer, Peter, Mantoulidis, Andreas, Phan, Jason, Smethurst, Christian A., Treu, Matthias, Waterson, Alex G., Lu, Hengyu, Machado, Annette, Daniele, Joseph, Fesik, Stephan W., Vellano, Christopher P., Heffernan, Timothy P., Marszalek, Joseph R., McConnell, Darryl B., Petronczki, Mark, Kraut, Norbert, Waizenegger, Irene C.
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Published in Cancer research (Chicago, Ill.) (01.07.2021)
Get full text
Journal Article
Discovery of Quinazolines as Histamine H-4 Receptor Inverse Agonists Using a Scaffold Hopping Approach
Smits, Rogier A., de Esch, Iwan J. P., Zuiderveld, Obbe P., Broeker, Joachim, Sansuk, Kamonchanok, Guaita, Elena, Coruzzi, Gabriella, Adami, Maristella, Haaksma, Eric, Leurs, Rob
Published in Journal of medicinal chemistry (25.12.2008)
Published in Journal of medicinal chemistry (25.12.2008)
Get full text
Journal Article
Targeted Synthesis of Complex Spiro[3H‐indole‐3,2′‐pyrrolidin]‐2(1H)‐ones by Intramolecular Cyclization of Azomethine Ylides: Highly Potent MDM2–p53 Inhibitors
Gollner, Andreas, Weinstabl, Harald, Fuchs, Julian E., Rudolph, Dorothea, Garavel, Geraldine, Hofbauer, Karin S., Karolyi‐Oezguer, Jale, Gmaschitz, Gerhard, Hela, Wolfgang, Kerres, Nina, Grondal, Elisabeth, Werni, Patrick, Ramharter, Juergen, Broeker, Joachim, McConnell, Darryl B.
Published in ChemMedChem (08.01.2019)
Published in ChemMedChem (08.01.2019)
Get full text
Journal Article
Targeted Synthesis of Complex Spiro3H-indole-3,2'-pyrrolidin-2(1H)-ones by Intramolecular Cyclization of Azomethine Ylides: Highly Potent MDM2-p53 Inhibitors
Gollner, Andreas, Weinstabl, Harald, Fuchs, Julian E, Rudolph, Dorothea, Garavel, Geraldine, Hofbauer, Karin S, Karolyi-Oezguer, Jale, Gmaschitz, Gerhard, Hela, Wolfgang, Kerres, Nina, Grondal, Elisabeth, Werni, Patrick, Ramharter, Juergen, Broeker, Joachim, McConnell, Darryl B
Published in ChemMedChem (08.01.2019)
Published in ChemMedChem (08.01.2019)
Get full text
Journal Article
Abstract A092: Determinants of sensitivity to BI KRASmulti inhibitor using high-throughput in-vitro drug screens
Schischlik, Fiorella, Tedeschi, Antonio, Rudolph, Dorothea, Gerlach, Daniel, Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Herdeis, Lorenz, Broeker, Joachim, Wunberg, Tobias, Boghossian, Andrew S., Rees, Matthew G., Ronan, Melissa M., Roth, Jennifer A., McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Haslinger, Christian, Lipp, Jesse
Published in Molecular cancer therapeutics (01.12.2023)
Published in Molecular cancer therapeutics (01.12.2023)
Get full text
Journal Article
암 치료를 위한 고리형 2-아미노-3-시아노 티오펜 및 유도체
GOLLNER ANDREAS, STADTMUELLER HEINZ, TREU MATTHIAS, LITTLE ANDREW, MANTOULIDIS ANDREAS, CUI JIANWEN, HODGES TIM, PHAN JASON, HERDEIS LORENZ, SMETHURST CHRISTIAN ALAN PAUL, WUNBERG TOBIAS, SARKAR DHRUBA, SOKOL KEVIN, WILDING BIRGIT, FUCHS JULIAN, WATERSON ALEX, FESIK STEPHEN W, BROEKER JOACHIM, RAMHARTER JUERGEN, ABBOTT JASON, SUN QI
Year of Publication 27.08.2024
Get full text
Year of Publication 27.08.2024
Patent
암 치료용 고리형 2-아미노-3-시아노 티오펜 및 유도체
GOLLNER ANDREAS, TREU MATTHIAS, LITTLE ANDREW, MANTOULIDIS ANDREAS, CUI JIANWEN, HODGES TIM, PHAN JASON, SMETHURST CHRISTIAN ALAN PAUL, SARKAR DHRUBA, WATERSON ALEX, FESIK STEPHEN W, BROEKER JOACHIM, KAROLYI OEZGUER JALE, ABBOTT JASON, SUN QI
Year of Publication 08.02.2023
Get full text
Year of Publication 08.02.2023
Patent
Abstract 3317: KRASmulti inhibitor BI 3706674 shows efficacy in KRAS-driven preclinical models of cancer that supports clinical testing in patients with tumors harbouring KRASG12V mutations and KRAS wild-type amplifications
Tedeschi, Antonio, Peng, David H., Schischlik, Fiorella, Herdeis, Lorenz, Schaaf, Otmar, Santoro, Valeria, Gerlach, Daniel, Savarese, Fabio, Lipp, Jesse, Haslinger, Christian, Rocchetti, Francesca, Popow, Johannes, Huber, Heinrich J., Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Broeker, Joachim, Wunber, Tobias, Gmachl, Michael, Rumpel, Klaus, Rees, Matthew, Ron, Melissa, Roth, Jennifer, Williams, Mariah, Deckard, Charles, Ramamoorthy, Vandhana, Daniele, Joseph R., Ajani, Jaffer A., Meric-Bernstam, Funda, Kopetz, Scott, Kim, Michael, Gibbons, Don L., Vellano, Christopher P., Marszalek, Joseph R., Heffernan, Timothy P., McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Rudolph, Dorothea
Published in Cancer research (Chicago, Ill.) (22.03.2024)
Published in Cancer research (Chicago, Ill.) (22.03.2024)
Get full text
Journal Article
Chiral linker. Part 3: Synthesis and evaluation of aryl substituted m-hydrobenzoins as solid supported open chain chiral auxiliaries for the diastereoselective reduction of α-keto esters
Broeker, Joachim, Knollmueller, Max, Gaertner, Peter
Published in Tetrahedron: asymmetry (25.09.2006)
Published in Tetrahedron: asymmetry (25.09.2006)
Get full text
Journal Article
MDM2-P53 억제제로서의 스피로[3H-인돌-3,2'-피롤리딘]-2(1H)-온 화합물 및 유도체
GOLLNER ANDREAS, WEINSTABL HARALD, HUCHLER GUENTHER, GOEPPER STEFAN, KERRES NINA, HENRY MANUEL, KOFINK CHRISTIANE, GILLE ANNIKA, BROEKER JOACHIM, RAMHARTER JUERGEN
Year of Publication 01.06.2018
Get full text
Year of Publication 01.06.2018
Patent
Synthesis of novel chiral hydrobenzoin mono- tert-butyl ethers derived from m-hydrobenzoin and their application as chiral auxiliaries in the diastereoselective reduction of α-keto esters
Schuster, Christian, Broeker, Joachim, Knollmueller, Max, Gaertner, Peter
Published in Tetrahedron: asymmetry (01.08.2005)
Published in Tetrahedron: asymmetry (01.08.2005)
Get full text
Journal Article