Development of potent dual PDK1/AurA kinase inhibitors for Ewing sarcoma therapy

被引:0
|
作者
Riveiro, Maria Eugenia [1 ]
Huguet, Samuel [2 ]
Vazquez, Ramiro [1 ]
Frapolli, Roberta [3 ]
Puricelli, Guido [4 ]
Sestito, Simona [5 ]
Madar, Olivier [2 ]
Rezai, Keyvan [2 ]
Garau, Gianpiero [6 ]
Rapposelli, Simona [7 ]
机构
[1] Early Drug Dev Grp, Boulogne, France
[2] Curie Inst, St Cloud, France
[3] Ist Ric Farmacol Mario Negri IRCCS, Milan, Italy
[4] Int Soc Drug Discovery, Milan, Italy
[5] Univ Sassari, Sassari, Italy
[6] Ist Italiano Tecnol, Pisa, Italy
[7] Univ Pisa, Pisa, Italy
关键词
D O I
暂无
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
2569
引用
收藏
页数:2
相关论文
共 50 条
  • [1] Development of potent dual PDK1/AurA kinase inhibitors for cancer therapy: Lead-optimization, structural insights, and ADME-Tox profile
    Sestito, Simona
    Bacci, Andrea
    Chiarugi, Sara
    Runfola, Massimiliano
    Gado, Francesca
    Margheritis, Eleonora
    Gul, Sheraz
    Riveiro, Maria E.
    Vazquez, Ramiro
    Huguet, Samuel
    Manera, Clementina
    Rezai, Keyvan
    Garau, Gianpiero
    Rapposelli, Simona
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2021, 226
  • [2] PDK1 inhibitors
    Barile, Elisa
    De, Surya K.
    Pellecchia, Maurizio
    PHARMACEUTICAL PATENT ANALYST, 2012, 1 (02) : 145 - 163
  • [3] Discovery of Novel, Potent, and Selective Inhibitors of 3-Phosphoinositide-Dependent Kinase (PDK1)
    Murphy, Sean T.
    Alton, Gordon
    Bailey, Simon
    Baxi, Sangita M.
    Burke, Benjamin J.
    Chappie, Thomas A.
    Ermolieff, Jacques
    Ferre, RoseAnn
    Greasley, Samantha
    Hickey, Michael
    Humphrey, John
    Kablaoui, Natasha
    Kath, John
    Kazmirski, Steven
    Kraus, Michelle
    Kupchinsky, Stan
    Li, John
    Lingardo, Laura
    Marx, Matthew A.
    Richter, Dan
    Tanis, Steven P.
    Tran, Khanh
    Vernier, William
    Xie, Zhi
    Yin, Min-Jean
    Yu, Xiao-Hong
    JOURNAL OF MEDICINAL CHEMISTRY, 2011, 54 (24) : 8490 - 8500
  • [4] Structure-based optimization of potent PDK1 inhibitors
    Angiolini, Mauro
    Banfi, Patrizia
    Casale, Elena
    Casuscelli, Francesco
    Fiorelli, Claudio
    Saccardo, Maria B.
    Silvagni, Marco
    Zuccotto, Fabio
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2010, 20 (14) : 4095 - 4099
  • [5] Selective 3-Phosphoinositide-Dependent Kinase 1 (PDK1) Inhibitors: Dissecting the Function and Pharmacology of PDK1
    Medina, Jesus R.
    JOURNAL OF MEDICINAL CHEMISTRY, 2013, 56 (07) : 2726 - 2737
  • [6] Novel, potent and selective small molecule inhibitors of 3-phosphoinositide-dependent kinase (PDK1)
    Murphy, Sean T.
    Alton, Gordon
    Bailey, Simon
    Baxi, Sangita
    Burke, Ben
    Ermolieff, Jacques
    Greasley, Samantha
    Kablaoui, Natasha
    Kath, John
    Kohls, Darcy
    Kothe, Michael
    Kupchinsky, Stan
    Lingardo, Laura
    Marx, Matthew A.
    Richter, Dan
    Khanh Tran
    Vernier, William
    Yin, Min-Jean
    CANCER RESEARCH, 2010, 70
  • [7] Development of the First Generation of Disulfide-Based Subtype Selective and Potent Covalent Pyruvate Dehydrogenase Kinase 1 (PDK1) Inhibitors
    Liu, Yifu
    Xie, Zuoquan
    Zhao, Dan
    Zhu, Jin
    Mao, Fei
    Tang, Shuai
    Xu, Hui
    Luo, Cheng
    Geng, Meiyu
    Huang, Min
    Li, Jian
    JOURNAL OF MEDICINAL CHEMISTRY, 2017, 60 (06) : 2227 - 2244
  • [8] Dual PDK1/Aurora Kinase A Inhibitors Reduce Pancreatic Cancer Cell Proliferation and Colony Formation
    Casari, Ilaria
    Domenichini, Alice
    Sestito, Simona
    Capone, Emily
    Sala, Gianluca
    Rapposelli, Simona
    Falasca, Marco
    CANCERS, 2019, 11 (11)
  • [9] Master kinase PDK1 in tumorigenesis
    Zheng, Nana
    Wei, Jiaqi
    Wu, Depei
    Xu, Yang
    Guo, Jianping
    BIOCHIMICA ET BIOPHYSICA ACTA-REVIEWS ON CANCER, 2023, 1878 (06):
  • [10] Discovery of 2-aminophenyl quinazolines as potent and selective PDK1 inhibitors
    Lin, Xiaodong
    Aikawa, Mina
    Amiri, Payman
    Basham, Steve
    Chan, Julie
    Jain, Rama
    Lin, Song
    Machajewsky, Timothy
    McCrea, William
    Menezes, Daniel
    Murray, Jeremy
    Ng, Simon
    Pfister, Keith
    Rico, Alice C.
    Ramurthy, Savithri
    Shu, Wei
    Subramanian, Sharadha
    Sutton, James
    Venetsanakos, Eleni
    Wang, Michael X.
    Warne, Bob
    Xu, Yongjin
    Zang, Richard
    Zhou, Yasheen
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2010, 240