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Chemistry, Medicinal
Pei-Ru Jin, Yen-Nhi Ngoc Ta, I-Ting Chen, Yan-Ning Yu, Hsin Tzu Hsieh, Van-Anh Thi Nguyen, Shang-Ying Hsieh, Tiffaney Hsia, Hao Liu, Chan-Wei Hsu, Jeng-Liang Han, Yunching Chen
Summary: The cinchona alkaloid derivative C1 exhibited potential cytotoxicity and inhibited autophagy in hepatocellular carcinoma cells, inducing apoptosis and blocking autophagy through the suppression of the Akt/mTOR/S6k pathway. Encapsulation of C1 into PEGylated PLGA nanoscale drug carriers significantly suppressed tumor growth and prevented metastasis, making it a promising therapeutic option for HCC.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
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Chemistry, Organic
Ting Chen, Jin-Tian Ma, Xiang-Long Chen, You Zhou, Zhi-Cheng Yu, Shuang-Gui Lei, Yan-Dong Wu, Jia-Chen Xiang, An-Xin Wu
Summary: We report a highly efficient one-pot, four-component reaction mediated by I-2-DMSO to construct a multifunctional fused system. This approach allows for selective formation of aromatics and non-aromatics under temperature control, resulting in planar and non-planar tetracyclic architectures that can be converted using simple methods.
ORGANIC CHEMISTRY FRONTIERS
(2023)
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Chemistry, Organic
Wen-Lin Zou, Yan-Qing Liu, Qing-Zhu Li, Xin-Xin Kou, Hua Huang, Rong-Sheng Tong, Jun-Long Li, Bo Han
Summary: In this study, an asymmetric dearomative tandem annulation between 3-nitroindoles and 7-oxo-5-heptenals was described. The cascade reactions proceeded smoothly using modularly designed organocatalysts self-assembled from cinchona-squaramide and d-proline. As a result, a collection of enantioenriched indoline-fused bicyclo[2.2.2]octanes featuring six vicinal stereocenters were smoothly obtained in good yields with excellent enantioselectivities (up to >99% ee). This protocol provides an economical and practical approach for the asymmetric synthesis of structurally complex indolines.
ORGANIC CHEMISTRY FRONTIERS
(2023)
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Biochemistry & Molecular Biology
Yu Dong, Liang-Xian Luo, Chen Hua, Ze-Jing He, Yong Chen, Zhi-Chuan Shi, Zhong-Hui Li, Bing He
Summary: In this study, a three-component tandem Michael addition/D-A cycloaddition reaction was successfully carried out without using any catalyst or organic solvent at 80°C in water. This reaction provides an easy access to polycyclic N-heterocycles derivatives containing indole and maleimide from readily available starting materials with moderate to high yields (up to 91%). Compared to conventional reaction conditions, this reaction not only enhances the efficiency and rate but also reduces the occurrence of side reactions.
CHEMISTRY & BIODIVERSITY
(2023)
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Medicine, Research & Experimental
Yael Babichev, Leah Kabaroff, Alessandro Datti, David Uehling, Methvin Isaac, Rima Al-awar, Michael Prakesch, Ren X. Sun, Paul C. Boutros, Rosemarie Venier, Brendan C. Dickson, Rebecca A. Gladdy
JOURNAL OF TRANSLATIONAL MEDICINE
(2016)
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Nanoscience & Nanotechnology
Md Badruz Zaman, David Bardelang, Michael Prakesch, Donald M. Leek, Jean-Valere Naubron, Gordon Chan, Xiaohua Wu, John A. Ripmeester, Christopher I. Ratcliffe, Kui Yu
ACS APPLIED MATERIALS & INTERFACES
(2012)
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Biochemistry & Molecular Biology
Michael Prakesch, Krikor Bijian, Valerie Campagna-Slater, Sophie Quevillon, Reni Joseph, Chang-Qing Wei, Esther Sesmilo, Ayub Reayi, Rajamohan R. Poondra, Michael L. Barnes, Donald M. Leek, Bin Xu, Caroline Lougheed, Matthieu Schapira, Moulay Alaoui-Jamali, Prabhat Arya
BIOORGANIC & MEDICINAL CHEMISTRY
(2008)
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Oncology
Douglas J. Mahoney, Charles Lefebvre, Kristina Allan, Jan Brun, Cina A. Sanaei, Stephen Baird, Nelson Pearce, Susanna Groenberg, Brian Wilson, Mikael Prakesh, Ahmed Aman, Methvin Isaac, Ahmed Mamai, David Uehling, Rima Al-Awar, Theresa Falls, Tommy Alain, David F. Stojdl
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Oncology
Natalie Grinshtein, Alessandro Datti, Mayumi Fujitani, David Uehling, Michael Prakesch, Methvin Isaac, Meredith S. Irwin, Jeffrey L. Wrana, Rima Al-awar, David R. Kaplan
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Biochemical Research Methods
Agata M. Trzcinska-Daneluti, Leo Nguyen, Chong Jiang, Christopher Fladd, David Uehling, Michael Prakesch, Rima Al-awar, Daniela Rotin
MOLECULAR & CELLULAR PROTEOMICS
(2012)
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Chemistry, Organic
Shahriar Khadem, Konstantin A. Udachin, Gary D. Enright, Michael Prakesch, Prabhat Arya
TETRAHEDRON LETTERS
(2009)
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Multidisciplinary Sciences
Mario Sanches, Nicole M. Duffy, Manisha Talukdar, Nero Thevakumaran, David Chiovitti, Marella D. Canny, Kenneth Lee, Igor Kurinov, David Uehling, Rima Al-awar, Gennadiy Poda, Michael Prakesch, Brian Wilson, Victor Tam, Colleen Schweitzer, Andras Toro, Julie L. Lucas, Danka Vuga, Lynn Lehmann, Daniel Durocher, Qingping Zeng, John B. Patterson, Frank Sicheri
NATURE COMMUNICATIONS
(2014)
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Biochemistry & Molecular Biology
Punit Saraon, Jamie Snider, Yannis Kalaidzidis, Leanne E. Wybenga-Groot, Konstantin Weiss, Ankit Rai, Nikolina Radulovich, Luka Drecun, Nika Vuckovic, Adriana Vucetic, Victoria Wong, Brigitte Theriault, Nhu-An Pham, Jin H. Park, Alessandro Datti, Jenny Wang, Shivanthy Pathmanathan, Farzaneh Aboualizadeh, Anna Lyakisheva, Zhong Yao, Yuhui Wang, Babu Joseph, Ahmed Aman, Michael F. Moran, Michael Prakesch, Gennady Poda, Richard Marcellus, David Uehling, Miroslav Samarzija, Marko Jakopovic, Ming-Sound Tsao, Frances A. Shepherd, Adrian Sacher, Natasha Leighl, Anna Akhmanova, Rima Al-awar, Marino Zerial, Igor Stagljar
NATURE CHEMICAL BIOLOGY
(2020)
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Biochemistry & Molecular Biology
Nardin Nano, Francisca Ugwu, Thiago Seraphim, Tangzhi Li, Gina Azer, Methvin Isaac, Michael Prakesch, Leandro R. S. Barbosa, Carlos H. Ramos, Alessandro Datti, Walid A. Houry
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Biochemistry & Molecular Biology
Ganna Posternak, Xiaojing Tang, Pierre Maisonneuve, Ting Jin, Hugo Lavoie, Salima Daou, Stephen Orlicky, Theo Goullet de Rugy, Lauren Caldwell, Kin Chan, Ahmed Aman, Michael Prakesch, Gennady Poda, Pavel Mader, Cassandra Wong, Stefan Maier, Julia Kitaygorodsky, Brett Larsen, Karen Colwill, Zhe Yin, Derek F. Ceccarelli, Robert A. Batey, Mikko Taipale, Igor Kurinov, David Uehling, Jeff Wrana, Daniel Durocher, Anne-Claude Gingras, Rima Al-Awar, Marc Therrien, Frank Sicheri
NATURE CHEMICAL BIOLOGY
(2020)
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Chemistry, Medicinal
David E. Uehling, Babu Joseph, Kim Chan Chung, Andrew X. Zhang, Spencer Ler, Michael A. Prakesch, Gennady Poda, Julie Grouleff, Ahmed Aman, Taira Kiyota, Chungyee Leung-Hagesteijn, John David Konda, Richard Marcellus, Carly Griffin, Ratheesh Subramaniam, Ayome Abibi, Craig A. Strathdee, Methvin B. Isaac, Rima Al-Awar, Rodger E. Tiedemann
Summary: The study reveals that targeting GRK6 with small molecule inhibitors is a promising therapeutic approach for multiple myeloma, and identifies a potential novel compound, 18, with potent efficacy.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Correction
Chemistry, Medicinal
David E. Uehling, Babu Joseph, Kim Chan Chung, Andrew X. Zhang, Spencer Ler, Michael A. Prakesch, Gennady Poda, Julie Grouleff, Ahmed Aman, Taira Kiyota, Chungyee Leung-Hagesteijn, John David Konda, Richard Marcellus, Carly Griffin, Ratheesh Subramaniam, Ayome Abibi, Craig A. Strathdee, Methvin B. Isaac, Rima Al-Awar, Rodger E. Tiedemann
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Punit Saraon, Jamie Snider, Wiebke Schormann, Ankit Rai, Nikolina Radulovich, Maria Sanchez-Osuna, Jasmin Coulombe-Huntington, Caroline Huard, Mohammed Mohammed, Evelyne Lima-Fernandes, Brigitte Theriault, Levon Halabelian, Manuel Chan, Dhananjay Joshi, Luka Drecun, Zhong Yao, Shivanthy Pathmanathan, Victoria Wong, Anna Lyakisheva, Farzaneh Aboualizadeh, Li Niu, Fengling Li, Taira Kiyota, Ratheesh Subramanian, Babu Joseph, Ahmed Aman, Michael Prakesch, Methvin Isaac, Ahmed Mamai, Gennady Poda, Masoud Vedadi, Richard Marcellus, David Uehling, Natasha Leighl, Adrian Sacher, Miroslav Samarzija, Marko Jakopovic, Cheryl Arrowsmith, Mike Tyers, Ming-Sound Tsao, David Andrews, Rima Al-awar, Igor Stagljar
Summary: The small molecule EM166 was identified to inhibit mutant EGFR signalling and growth in NSCLC cells via a novel mechanism. EM166 affects the expression and signalling of certain proteins, alters subcellular localization, and modulates the ER stress response pathway in mutant EGFR lung cancer cells.
JOURNAL OF MOLECULAR BIOLOGY
(2021)