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Design and Synthesis of a 2-Amino-pyridine Derivative as a Potent CDK8 Inhibitor for Anti-colorectal Cancer Therapy

https://doi.org/10.1021/acs.jmedchem.2c01042
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What this work says

Outgoing claims: the papers this work cites, builds on, or argues with.

inferredcites →https://doi.org/10.1002/ijc.24908openalex-snapshot
CDK8 expression in 470 colorectal cancers in relation to β‐catenin activation, other molecular alterations and patient survival
inferredcites →https://doi.org/10.1002/med.21700openalex-snapshot
Recent updates on the resistance mechanisms to epidermal growth factor receptor tyrosine kinase inhibitors and resistance reversion strategies in lung cancer
inferredcites →https://doi.org/10.1007/978-3-319-91442-8_3openalex-snapshot
Regorafenib
inferredcites →https://doi.org/10.1007/s40265-018-0998-zopenalex-snapshot
Fruquintinib: First Global Approval
inferredcites →https://doi.org/10.1016/bs.podrm.2018.11.003openalex-snapshot
Sorafenib
inferredcites →https://doi.org/10.1016/j.addr.2020.12.010openalex-snapshot
Therapeutic targeting of the oncogenic Wnt signaling pathway for treating colorectal cancer and other colonic disorders
inferredcites →https://doi.org/10.1016/j.biochi.2013.10.004openalex-snapshot
The two faces of Cdk8, a positive/negative regulator of transcription
inferredcites →https://doi.org/10.1016/j.ejmech.2020.113043openalex-snapshot
Angel or Devil ? - CDK8 as the new drug target
inferredcites →https://doi.org/10.1016/j.immuni.2012.10.017openalex-snapshot
CDK8 Kinase Phosphorylates Transcription Factor STAT1 to Selectively Regulate the Interferon Response
inferredcites →https://doi.org/10.1016/j.jmb.2011.07.020openalex-snapshot
The Structure of CDK8/CycC Implicates Specificity in the CDK/Cyclin Family and Reveals Interaction with a Deep Pocket Binder
inferredcites →https://doi.org/10.1016/j.tibs.2005.03.002openalex-snapshot
The mammalian Mediator complex and its role in transcriptional regulation
inferredcites →https://doi.org/10.1016/j.tox.2013.07.013openalex-snapshot
Wogonin induced G1 cell cycle arrest by regulating Wnt/β-catenin signaling pathway and inactivating CDK8 in human colorectal cancer carcinoma cells
inferredcites →https://doi.org/10.1016/s0092-8674(00)00122-7openalex-snapshot
Linking Colorectal Cancer to Wnt Signaling
inferredcites →https://doi.org/10.1016/s0092-8674(02)01014-0openalex-snapshot
The β-Catenin/TCF-4 Complex Imposes a Crypt Progenitor Phenotype on Colorectal Cancer Cells
inferredcites →https://doi.org/10.1016/s0140-6736(05)17706-xopenalex-snapshot
Colorectal cancer
inferredcites →https://doi.org/10.1021/acs.jmedchem.5b01685openalex-snapshot
Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19
inferredcites →https://doi.org/10.1021/jm501436mopenalex-snapshot
Discovery of Potent, Orally Bioavailable, Small-Molecule Inhibitors of WNT Signaling from a Cell-Based Pathway Screen
inferredcites →https://doi.org/10.1038/359235a0openalex-snapshot
APC mutations occur early during colorectal tumorigenesis
inferredcites →https://doi.org/10.1038/521s1aopenalex-snapshot
Colorectal cancer
inferredcites →https://doi.org/10.1038/nature07179openalex-snapshot
CDK8 is a colorectal cancer oncogene that regulates β-catenin activity
inferredcites →https://doi.org/10.1038/nature07310openalex-snapshot
E2F1 represses β-catenin transcription and is antagonized by both pRB and CDK8
inferredcites →https://doi.org/10.1038/nchembio.1952openalex-snapshot
A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease
inferredcites →https://doi.org/10.1038/nrgastro.2011.173openalex-snapshot
Epigenetics and colorectal cancer
inferredcites →https://doi.org/10.1038/nsmb.2549openalex-snapshot
A conserved Mediator–CDK8 kinase module association regulates Mediator–RNA polymerase II interaction
inferredcites →https://doi.org/10.1038/s41467-019-09898-0openalex-snapshot
MEK inhibitors activate Wnt signalling and induce stem cell plasticity in colorectal cancer
inferredcites →https://doi.org/10.1038/s41467-019-11721-9openalex-snapshot
Single-cell transcriptomics reveals multi-step adaptations to endocrine therapy
inferredcites →https://doi.org/10.1038/s41467-020-19173-2openalex-snapshot
5-FU promotes stemness of colorectal cancer via p53-mediated WNT/β-catenin pathway activation
inferredcites →https://doi.org/10.1046/j.1365-2362.2002.01004.xopenalex-snapshot
Molecular causes of colon cancer
inferredcites →https://doi.org/10.1073/pnas.1206906109openalex-snapshot
Cyclin-dependent kinase 8 mediates chemotherapy-induced tumor-promoting paracrine activities
inferredcites →https://doi.org/10.1074/jbc.m602696200openalex-snapshot
Mediator Is a Transducer of Wnt/β-Catenin Signaling
inferredcites →https://doi.org/10.1111/j.1365-2443.2007.01036.xopenalex-snapshot
A kinase subunit of the human mediator complex, CDK8, positively regulates transcriptional activation
inferredcites →https://doi.org/10.1126/stke.2712005cm1openalex-snapshot
Wnt/β-Catenin Pathway
inferredcites →https://doi.org/10.1158/1541-7786.mcr-06-0398openalex-snapshot
APC Mutations and Other Genetic and Epigenetic Changes in Colon Cancer
inferredcites →https://doi.org/10.1186/gb4184openalex-snapshot
Cyclin-dependent kinases
inferredcites →https://doi.org/10.1593/neo.04448openalex-snapshot
Genetic and Epigenetic Changes of Components Affecting the WNT Pathway in Colorectal Carcinomas Stratified by Microsatellite Instability
inferredcites →https://doi.org/10.18632/oncotarget.14894openalex-snapshot
Inhibition of CDK8 mediator kinase suppresses estrogen dependent transcription and the growth of estrogen receptor positive breast cancer
inferredcites →https://doi.org/10.3390/cells8111413openalex-snapshot
Systemic Toxicity Reported for CDK8/19 Inhibitors CCT251921 and MSC2530818 Is Not Due to Target Inhibition
inferredcites →https://doi.org/10.3390/cells9092125openalex-snapshot
Transcriptional Regulation of Wnt/β-Catenin Pathway in Colorectal Cancer
inferredcites →https://doi.org/10.3390/ijms21155343openalex-snapshot
The Role of CDKs and CDKIs in Murine Development
inferredcites →https://doi.org/10.4161/cbt.11.9.15050openalex-snapshot
Molecular mechanisms of resistance to the EGFR monoclonal antibody cetuximab

What points at this work

Incoming claims: where this work appears in other papers’ reference lists and arguments.

inferred← citeshttps://doi.org/10.2139/ssrn.4760318openalex-extracted
inferred← citeshttps://doi.org/10.1016/j.bbadis.2023.166880openalex-snapshot
Small-molecule drugs of colorectal cancer: Current status and future directions
inferred← citeshttps://doi.org/10.1016/j.bbadis.2025.167899openalex-snapshot
Characterization and targeting of chemoresistant triple-negative breast cancer subtypes using amino-pyridine compounds
inferred← citeshttps://doi.org/10.1016/j.bcp.2026.117916openalex-snapshot
Discovery and research progress of CDK8 inhibitors
inferred← citeshttps://doi.org/10.1016/j.bmc.2025.118287openalex-snapshot
A comprehensive description of cyclin-dependent kinase 8 (CDK8) inhibitors as anticancer agents
inferred← citeshttps://doi.org/10.1016/j.bmcl.2026.130711openalex-snapshot
Design, synthesis and biological evaluation of novel CDK8/BRD4 dual inhibitors
inferred← citeshttps://doi.org/10.1016/j.ejmech.2024.116547openalex-snapshot
Targeting cyclin-dependent kinases: From pocket specificity to drug selectivity
inferred← citeshttps://doi.org/10.1016/j.fitote.2024.105967openalex-snapshot
Four sulfur-containing compounds with anti-colon cancer effect from marine-derived fungus Aspergillus terreus
inferred← citeshttps://doi.org/10.1016/j.jare.2025.01.017openalex-snapshot
CDK8 mediated inflammatory microenvironment aggravates osteoarthritis progression
inferred← citeshttps://doi.org/10.1016/j.molliq.2024.125682openalex-snapshot
Elucidation of the solution structure of macrocyclic paritaprevir and exploration of its antitumor potential through molecular docking
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.4c00248openalex-snapshot
Discovery of a Novel and Potent Cyclin-Dependent Kinase 8/19 (CDK8/19) Inhibitor for the Treatment of Cancer
inferred← citeshttps://doi.org/10.1021/acs.jmedchem.4c03226openalex-snapshot
Discovery of Potent and Balanced Dual RIPK2 and 3 Inhibitors as a New Strategy for the Treatment of Inflammatory Bowel Diseases
inferred← citeshttps://doi.org/10.1021/acs.molpharmaceut.6c00563openalex-snapshot
GenMAS: A Machine Learning-Based Modeling and Assessment Strategy for ADMET Profiling and its Application in PBPK Simulation
inferred← citeshttps://doi.org/10.1039/d4md00465eopenalex-snapshot
Design and synthesis of 7-azaindole derivatives as potent CDK8 inhibitors for the treatment of acute myeloid leukemia
inferred← citeshttps://doi.org/10.1039/d4ra07438fopenalex-snapshot
Cracking the code: the clinical and molecular impact of aminopyridines; a review (2019–2024)
inferred← citeshttps://doi.org/10.1039/d6md00281aopenalex-snapshot
Discovery of a potent dual-target CDK8 and cyclin C PROTAC degrader for the treatment of colorectal cancer
inferred← citeshttps://doi.org/10.1080/14756366.2024.2305852openalex-snapshot
Discovery of novel and potent CDK8 inhibitors for the treatment of acute myeloid leukaemia
inferred← citeshttps://doi.org/10.14295/bjs.v5i3.825openalex-snapshot
Intramolecular interaction analysis of forty amine derivatives with phosphodiesterase 4D using a theoretical model
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