Cover Image

Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyridazinone derivatives as covalent FGFR inhibitors

Fibroblast growth factor receptors (FGFRs) have emerged as promising targets for anticancer therapy. In this study, we synthesized and evaluated the biological activity of 66 pyrazolo[3,4-d]pyridazinone derivatives. Kinase inhibition, cell proliferation, and whole blood stability assays were used to...

Full description

Saved in:

Bibliographic Details
Main Authors:	Xiaowei Wu (Author), Mengdi Dai (Author), Rongrong Cui (Author), Yulan Wang (Author), Chunpu Li (Author), Xia Peng (Author), Jihui Zhao (Author), Bao Wang (Author), Yang Dai (Author), Dan Feng (Author), Tianbiao Yang (Author), Hualiang Jiang (Author), Meiyu Geng (Author), Jing Ai (Author), Mingyue Zheng (Author), Hong Liu (Author)
Format:	Book
Published:	Elsevier, 2021-03-01T00:00:00Z.
Subjects:	article
Online Access:	Connect to this object online.
Tags:	Add Tag No Tags, Be the first to tag this record!

Similar Items

Studies on new substituted pyridazinones: synthesis and biological evaluation
by: Mohammad Asif, et al.
Published: (2018)

Pyrazolo[3,4-d]pyrimidine based scaffold derivatives targeting kinases as anticancer agents
by: Nasser S.M. Ismail, et al.
Published: (2016)

Repurposing strategies on pyridazinone-based series by pharmacophore- and structure-driven screening
by: Giuseppe Floresta, et al.
Published: (2020)

Identification of 1H-pyrazolo[3,4-b]pyridine derivatives as potent ALK-L1196M inhibitors
by: Yunju Nam, et al.
Published: (2019)

A PYRAZOLO[3,4-d]PYRIMIDINE COMPOUND REDUCES CELL VIABILITY AND INDUCES APOPTOSIS IN DIFFERENT HEMATOLOGICAL MALIGNANCIES
by: Ilaria Laurenzana, et al.
Published: (2016)

Halloysite Nanotube-Based Delivery of Pyrazolo[3,4-<i>d</i>]pyrimidine Derivatives for Prostate and Bladder Cancer Treatment
by: Marina Massaro, et al.
Published: (2024)

Synthesis of some novel pyrazolo[3,4-d] pyrimidin-4(5H)-one derivatives as potential antimicrobial agent
by: Dipen K Sureja, et al.
Published: (2016)

Identification and Biological Characterization of the Pyrazolo[3,4-<i>d</i>]pyrimidine Derivative SI388 Active as Src Inhibitor
by: Claudia Contadini, et al.
Published: (2023)

Novel 1,3,4-Oxadiazole Derivatives of Pyrrolo[3,4-d]Pyridazinone Exert Anti-Inflammatory Activity without Acute Gastrotoxicity in the Carrageenan-Induced Rat Paw Edema Test
by: Szandruk-Bender M, et al.
Published: (2021)

Highlight on lipids and its use for covalent and non-covalent conjugations
by: Abdullah Q. Khudhur, et al.
Published: (2020)

Design, ADMET, PASS Prediction and Molecular Docking Studies of Novel pyrazolo[3,4-d]pyrimidines for Prospective of Anti-Cancer Agents
by: Sathish Mittapalli, et al.
Published: (2023)

Novel Glu-based pyrazolo[3,4-d]pyrimidine analogues: design, synthesis and biological evaluation as DHFR and TS dual inhibitors
by: Mater Mahnashi, et al.
Published: (2023)

Discovery of new 1H-pyrazolo[3,4-d]pyrimidine derivatives as anticancer agents targeting EGFRWT and EGFRT790M
by: Ahmed A. Gaber, et al.
Published: (2022)

Synthesis, biological evaluation, and in silico studies of new CDK2 inhibitors based on pyrazolo[3,4-d]pyrimidine and pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine scaffold with apoptotic activity
by: Asmaa A. Mandour, et al.
Published: (2022)

Targeting p21-activated kinase 4 (PAK4) with pyrazolo[3,4-d]pyrimidine derivative SPA7012 attenuates hepatic ischaemia-reperfusion injury in mice
by: Yuancheng Mao, et al.
Published: (2022)

Design, synthesis and antitumor evaluation of novel pyrazolo[3,4-d]pyrimidines incorporating different amino acid conjugates as potential DHFR inhibitors
by: Ibrahim M. Salem, et al.
Published: (2023)

The Role of Pyrazolo[3,4-d]pyrimidine-Based Kinase Inhibitors in The Attenuation of CCl<sub>4</sub>-Induced Liver Fibrosis in Rats
by: Diana K. Ghobrial, et al.
Published: (2023)

Identification of 1H-pyrazolo[3,4-b]pyridine derivatives as novel and potent TBK1 inhibitors: design, synthesis, biological evaluation, and molecular docking study
by: Yin Sun, et al.
Published: (2022)

Covalent Organic Frameworks
Published: (2023)

Anti-Diabetic Activities and Molecular Docking Studies of Aryl-Substituted Pyrazolo[3,4-b]pyridine Derivatives Synthesized via Suzuki Cross-Coupling Reaction
by: Iqra Rafique, et al.
Published: (2024)

Design and synthesis of novel pyrazolo[4,3-d]pyrimidines as potential therapeutic agents for acute lung injury
by: Bao Shi Wang, et al.
Published: (2019)

Effect of FGFR alteration on prognosis in 1963 urothelial carcinoma patients with immune checkpoint inhibitors: Implying combination of FGFR inhibitor and immunotherapy for FGFR-altered urothelial carcinoma
by: Yuxuan Song, et al.
Published: (2024)

Discovery of a subtype-selective, covalent inhibitor against palmitoylation pocket of TEAD3
by: Tian Lu, et al.
Published: (2021)

Biological Evaluation and In Vitro Characterization of ADME Profile of In-House Pyrazolo[3,4-<i>d</i>]pyrimidines as Dual Tyrosine Kinase Inhibitors Active against Glioblastoma Multiforme
by: Federica Poggialini, et al.
Published: (2023)

Novel Pyrazolo[3,4-b] Pyridine Derivative (HLQ2g) Attenuates Hypoxic Pulmonary Hypertension via Restoring cGKI Expression and BMP Signaling Pathway
by: Lijun Li, et al.
Published: (2021)

Recent Advances in Covalent Drug Discovery
by: Daniel Schaefer, et al.
Published: (2023)

New Pyrazolo-Benzimidazole Mannich Bases with Antimicrobial and Antibiofilm Activities
by: Christina Zalaru, et al.
Published: (2022)

Somatic FGFR3 mutations in seborrheic keratosis and acanthosis nigricans of Chinese patients
by: Guiye Niu, et al.
Published: (2014)

Role of FGFR3 in Urothelial Carcinoma
by: Malik Akanksha, et al.
Published: (2019)

Induction of Paraptotic Cell Death in Breast Cancer Cells by a Novel Pyrazolo[3,4-<i>h</i>]quinoline Derivative through ROS Production and Endoplasmic Reticulum Stress
by: Phuong Linh Nguyen, et al.
Published: (2022)

Synthesis and properties of 3-(ethylthio)-9-methyl-6-(alkylthio)pyrazolo[1,5-d][1,2,4]triazolo[3,4-f][1,2,4]triazines
by: S. O. Fedotov, et al.
Published: (2022)

Effects of Intermittent Administration of Parathyroid Hormone (1-34) on Bone Differentiation in Stromal Precursor Antigen-1 Positive Human Periodontal Ligament Stem Cells
by: Xiaoxiao Wang, et al.
Published: (2016)

Distinct or Overlapping Areas of Mitochondrial Thioredoxin 2 May Be Used for Its Covalent and Strong Non-Covalent Interactions with Protein Ligands
by: Charalampos Ntallis, et al.
Published: (2023)

Non-covalent Interactions in Coordination and Organometallic Chemistry
Published: (2022)

Discovery of New 1,4,6-Trisubstituted-1<i>H</i>-pyrazolo[3,4-<i>b</i>]pyridines with Anti-Tumor Efficacy in Mouse Model of Breast Cancer
by: Maria Georgiou, et al.
Published: (2023)

Identification of covalent active site inhibitors of dengue virus protease
by: Koh-Stenta X, et al.
Published: (2015)

The Evaluation of <i>FGFR1</i>, <i>FGFR2</i> and <i>FOXO1</i> in Orofacial Cleft Tissue
by: Jana Goida, et al.
Published: (2022)

Discovery of a series of dimethoxybenzene FGFR inhibitors with 5H-pyrrolo[2,3-b]pyrazine scaffold: structure-activity relationship, crystal structural characterization and in vivo study
by: Peng Wei, et al.
Published: (2019)

Design, Synthesis, In Vitro, and In Silico Studies of New <i>N</i><sup>5</sup>-Substituted-pyrazolo[3,4-<i>d</i>]pyrimidinone Derivatives as Anticancer CDK2 Inhibitors
by: Waheed A. Zaki, et al.
Published: (2023)

A targeted covalent inhibitor of p97 with proteome-wide selectivity
by: Zi Ye, et al.
Published: (2022)