Discovery of pyrazolo[1,5-a]pyrimidin-7-amine derivatives as mTOR kinase domain inhibitors: Hit to lead optimization

被引:0
|
作者
Deng, Yongqi [1 ]
Sun, Binyuan [1 ]
Shipps, Gerald [1 ]
Matthew, Richards [1 ]
Meng, Zhaoyang [1 ]
Windsor, Williama [1 ]
Zeng, Hongbo [1 ]
Long, Brian [1 ]
Xiao, Li [1 ]
机构
[1] Merck Res Labs, Drug Discovery, Boston, MA 02115 USA
来源
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY | 2014年 / 248卷
关键词
D O I
暂无
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
165-MEDI
引用
收藏
页数:1
相关论文
共 50 条
  • [21] Discovery and structure - activity relationship exploration of pyrazolo [1,5-a]pyrimidine derivatives as potent FLT3-ITD inhibitors
    Chen, Yun
    Bai, Gang
    Li, Yan
    Ning, Yi
    Cao, Sufen
    Zhou, Jinpei
    Ding, Jian
    Zhang, Huibin
    Xie, Hua
    Duan, Wenhu
    BIOORGANIC & MEDICINAL CHEMISTRY, 2021, 48
  • [22] Highly selective C3-sulfenylation and C3-selenylation of 3-iodo-5-arylpyrazolo[1,5-a]pyrimidin-7-amine in water
    Sang, Tian
    Jia, Fan
    He, Jing
    Liu, Yan
    Liu, Jichang
    Liu, Ping
    JOURNAL OF MOLECULAR STRUCTURE, 2023, 1292
  • [23] Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma
    Mathison, Casey J. N.
    Chianelli, Donatella
    Rucker, Paul V.
    Nelson, John
    Roland, Jason
    Huang, Zhihong
    Yang, Yang
    Jiang, Jiqing
    Xie, Yun Feng
    Epple, Robert
    Bursulaya, Badry
    Lee, Christian
    Gao, Mu-Yun
    Shaffer, Jennifer
    Briones, Sergio
    Sarkisova, Yelena
    Galkin, Anna
    Li, Lintong
    Li, Nanxin
    Li, Chun
    Hua, Su
    Kasibhatla, Shailaja
    Kinyamu-Akunda, Jacqueline
    Kikkawa, Rie
    Molteni, Valentina
    Tellew, John E.
    ACS MEDICINAL CHEMISTRY LETTERS, 2020, 11 (04): : 558 - 565
  • [24] Advances in pyrazolo[1,5-a]pyrimidines: synthesis and their role as protein kinase inhibitors in cancer treatment
    Iorkula, Terungwa H.
    Jude-Kelly Osayawe, Osasere
    Odogwu, Daniel A.
    Ganiyu, Latifat Oluwatobi
    Faderin, Emmanuel
    Awoyemi, Raymond Femi
    Akodu, Busayo Odunayo
    Ifijen, Ikhazuagbe Hilary
    Aworinde, Omowunmi Rebecca
    Agyemang, Peter
    Onyinyechi, Odo Lovelyn
    RSC ADVANCES, 2025, 15 (05) : 3756 - 3828
  • [25] Synthesis and Bioactivity of Pyrazolo[1,5-a]pyrimidine Derivatives as Novel c-Met Inhibitors
    Ni, Chunyan
    Zhang, Yuting
    Zhao, Yu
    Zhu, Li
    CHINESE JOURNAL OF ORGANIC CHEMISTRY, 2012, 32 (12) : 2294 - 2299
  • [26] Synthesis of pyrazolo[1,5-a][1,3,5]triazine derivatives as inhibitors of thymidine phosphorylase
    Sun, Lingyi
    Bera, Hriday
    Chui, Wai Keung
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2013, 65 : 1 - 11
  • [27] Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors:: Improvements in physical properties enhance cellular activity and pharmacokinetics
    Fraley, ME
    Rubino, RS
    Hoffman, WF
    Hambaugh, SR
    Arrington, KL
    Hungate, RW
    Bilodeau, MT
    Tebben, AJ
    Rutledge, RZ
    Kendall, RL
    McFall, RC
    Huckle, WR
    Coll, KE
    Thomas, KA
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2002, 12 (24) : 3537 - 3541
  • [28] Preparation and optimization of pyrazolo[1,5-a]pyrimidines as new potent PDE4 inhibitors
    Le Roux, Jacques
    Leriche, Caroline
    Chamiot-Clerc, Philippe
    Feutrill, John
    Halley, Frank
    Papin, David
    Derimay, Nathalie
    Mugler, Christelle
    Grepin, Claudine
    Schio, Laurent
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2016, 26 (02) : 454 - 459
  • [29] Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: A template-based approach
    Dwyer, Michael P.
    Keertikar, Kartik
    Paruch, Kamil
    Alvarez, Carmen
    Labroli, Marc
    Poker, Cory
    Fischmann, Thierry O.
    Mayer-Ezell, Rosemary
    Bond, Richard
    Wang, Yan
    Azevedo, Rita
    Guzi, Timothy J.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2013, 23 (22) : 6178 - 6182
  • [30] Discovery of 3-pyrazolyl-substituted pyrazolo[1,5-a]pyrimidine derivatives as potent TRK inhibitors to overcome clinically acquired resistance
    Gong, Yi
    Wu, Feng-Xu
    Wang, Ming-Shu
    Xu, Hong-Chuang
    Zhuo, Lin-Sheng
    Yang, Guang-Fu
    Huang, Wei
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2022, 241