Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Plewe Michael Bruno"'
Autor:
Matthew R. Lee, Yang Xu, Chao Zhang, Weihua Yu, Liqun Chen, Bingyang Jiao, Ying Luo, Plewe Michael Bruno, Lei Sun, Jialiang Wang, Yanke Chen, Yuanqi Wei, Tingting Shi, Xiaoran Han, Chunyan Zhang
Publikováno v:
Journal of Medicinal Chemistry. 63:4069-4080
BRAF is among the most frequently mutated oncogenes in human cancers. Multiple small molecule BRAF kinase inhibitors have been approved for treating melanoma carrying BRAF-V600 mutations. However, the benefits of BRAF kinase inhibitors are generally
Autor:
Qiong Tan, Yanke Chen, Plewe Michael Bruno, Xiaoran Han, Wuyi Yao, Sheng Liang, Hongyu Chai, Chunyan Zhang, Jianguo Yu, Bingyang Jiao, Weihua Yu, Hui Yang, Jing Liu, Liqun Chen, Ying Luo, Yongzheng Qian, Jialiang Wang
Publikováno v:
Journal of medicinal chemistry. 63(23)
We report compounds 5 (CG416) and 6 (CG428) as two first-in-class tropomyosin receptor kinase (TRK) degraders that target the intracellular kinase domain of TRK. Degraders 5 and 6 reduced levels of the tropomyosin 3 (TPM3)-TRKA fusion protein in KM12
Autor:
Eric Brown, E. Adam Kallel, Donald D. Lorimer, Arshil Master, Ken McCormack, Alexandra Fetsko, David M. Dranow, Nadezda V. Sokolova, Rana Sidhu, Alexander N. Freiberg, Vidyasagar Reddy Gantla, Plewe Michael Bruno, Jameson Bullen, Greg Henkel, Junru Wang, Shibani Naik, Birte Kalveram, Hayden Smutney, Lihong Zhang
Publikováno v:
ACS Med Chem Lett
[Image: see text] We identified and explored the structure–activity-relationship (SAR) of an adamantane carboxamide chemical series of Ebola virus (EBOV) inhibitors. Selected analogs exhibited half-maximal inhibitory concentrations (EC(50) values)
Autor:
Birte Kalveram, Alexander N. Freiberg, Eric Brown, Nadezda V. Sokolova, Greg Henkel, Shibani Naik, Ken McCormack, Alexandra Fetsko, Young-Jun Shin, Vidyasagar Reddy Gantla, Lihong Zhang, Plewe Michael Bruno
Publikováno v:
Bioorg Med Chem Lett
We identified and explored the structure–activity relationship (SAR) of a novel heterocyclic chemical series of arenavirus cell entry inhibitors. Optimized lead compounds, including diphenyl-substituted imidazo[1,2-a]pyridines, benzimidazoles, and
Autor:
Eric Brown, Vidyasagar Reddy Gantla, Landon R. Whitby, Ken McCormack, Joanne York, Dale L. Boger, Plewe Michael Bruno, Birte Kalveram, Jack H. Nunberg, Greg Henkel, Alexander N. Freiberg, Nadezda V. Sokolova, Shibani Naik, Lihong Zhang
Publikováno v:
Bioorg Med Chem Lett
Old World (Africa) and New World (South America) arenaviruses are associated with human hemorrhagic fevers. Efforts to develop small molecule therapeutics have yielded several chemical series including the 4-acyl-1,6-dialkylpiperazin-2-ones. Herein,
Autor:
Jing Liu, Xiaoran Han, Liqun Chen, Bingyang Jiao, Jialiang Wang, Chengwei Zhang, Yanke Chen, Plewe Michael Bruno
Publikováno v:
Cancer Research. 80:5331-5331
Small molecule-mediated targeted protein degradation offers a systemic approach to deplete disease-causing proteins. The tropomyosin receptor kinase (TRK) family kinases are receptors for neurotrophic factors and primarily function in the central ner
Autor:
Eric Zhang, Shubha Bagrodia, Phuong Le, Hai Wang, Daniel R. Knighton, Cheng Hengmiao, Plewe Michael Bruno, Sacha Ninkovic, Samantha Elizabeth Greasley, Shaoxian Sun, Caroline M. LaFleur Rogers, Andrew Pannifer, Xiaojun Huang, Deepak Dalvie
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5098-5103
Lead optimization efforts that employed structure base drug design and physicochemical property based optimization leading to the discovery of a novel series of 4-methylpyrido pyrimidinone (MPP) are discussed. Synthesis and profile of 1, a PI3Kα/mTO
Autor:
Tran Khanh Tuan, Qiyue Hu, Zhang Junhu, Scott L. Butler, Atsuo Kuki, Qinghai Peng, Erik Jon Flahive, Graham L. Smith, Huichun Zhu, Deepak Dalvie, Plewe Michael Bruno, Jim Solowiej, Dorothy Delisle, Ted William Johnson, Wen Liu, Steven P. Tanis, Klaus Ruprecht Dress, Jon E. Kuehler, Guy A. McClellan, Xiaoming Yu, Hai Wang, Paul F. Richardson
Publikováno v:
Journal of Medicinal Chemistry. 54:3393-3417
HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential for viral replication, and HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Recently, we reported the synthesis of orally bioavailable a
Autor:
Qinghai Peng, Tran Khanh Tuan, Atsuo Kuki, Steven P. Tanis, Zhang Junhu, Deepak Dalvie, Yang Anle, Xiaoming Yu, Jim Solowiej, Ted William Johnson, Hai Wang, Wen Liu, Plewe Michael Bruno, Buwen Huang, Graham L. Smith, Jon E. Kuehler, Klaus Ruprecht Dress, Chunfeng Yin, Qiyue Hu, Dorothy Delisle, Huichun Zhu, Scott L. Butler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:7429-7434
HIV-1 integrase is one of three enzymes encoded by the HIV genome and is essential for viral replication, and HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Recently, we reported the discovery of azaindole hydroxamic acids
Autor:
Qinghai Peng, Nowlin Dawn Marie, Hieu Lam, Ted William Johnson, Yang Anle, Wen Liu, Atsuo Kuki, Steven P. Tanis, Jon E. Kuehler, Zhang Junhu, Hai Wang, Plewe Michael Bruno, Scott L. Butler, Tran Khanh Tuan, Qiyue Hu, Sadayappan V. Rahavendran, Klaus Ruprecht Dress
Publikováno v:
Journal of Medicinal Chemistry. 52:7211-7219
HIV-1 integrase (IN) is one of three enzymes encoded by the HIV genome and is essential for viral replication. Recently, HIV-1 IN inhibitors have emerged as a new promising class of therapeutics. Herein, we report the discovery of azaindole carboxyli