Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.

No abstract is available for this paper.

• Publication year

  2004

• Venue

  Journal of Medicinal Chemistry

• Publication date

  2004-12-07

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1021/JM049486APMID 15615512
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Overriding Imatinib Resistance with a Novel ABL Kinase Inhibitor

  2004cited by this paper
• A novel pyridopyrimidine inhibitor of abl kinase is a picomolar inhibitor of Bcr-abl-driven K562 cells and is effective against STI571-resistant Bcr-abl mutants.

  2003cited by this paper
• Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).

  2003cited by this paper
• STI571 as a Targeted Therapy for CML

  2003cited by this paper
• Src in cancer: deregulation and consequences for cell behaviour.

  2002cited by this paper
• Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571).

  2001cited by this paper
• BMS-247550: a novel epothilone analog with a mode of action similar to paclitaxel but possessing superior antitumor efficacy.

  2001cited by this paper
• Crystal structures of c-Src reveal features of its autoinhibitory mechanism.

  1999cited by this paper

• Functional remodeling of iNKT cells by sulfatide-reactive type II NKT cells reprograms alveolar macrophages to alleviate lung ischemia-reperfusion injury

  2026cites this paper
• Expanding landscape of kinase inhibitor research in 25 years (2001-2025) and advancements of next-generation kinase inhibitors.

  2026cites this paper
• Identification of 3-cyanoquinolines as broad-spectrum inhibitors of Monkeypox virus and other sexually transmitted pathogens.

  2026cites this paper
• Bacterial ubiquitin ligase engineered for small molecule and protein target identification

  2026cites this paper
• Cellular Senescence, Inflammaging and Cardiovascular Disease

  2026cites this paper
• Toward the future management of patients with CML and Ph + ALL: real-world safety insights from dasatinib pharmacovigilance

  2026cites this paper
• Novel piperazine–pyrimidine hybrids as potential anticancer agents against MCF-7 breast carcinoma: synthesis, antimicrobial activity, antioxidant evaluation, and computational insights

  2026cites this paper
• Enhancing the Water Solubility and Efficacy of Anticancer Drugs Using Hydroxypropyl-β-Cyclodextrin

  2026cites this paper
• BCR-ABL Inhibitors in the Targeted Therapy of Chronic Myeloid Leukemia

  2025cites this paper
• Modulating the phosphorylation status of target proteins through bifunctional molecules.

  2025cites this paper
• CML stem cells and their interactions and adaptations to tyrosine kinase inhibitors

  2025cites this paper
• Targeting kinases that regulate programmed cell death: a new therapeutic strategy for breast cancer

  2025cites this paper
• uPAR-targeted senolytic delivery to enhance cancer therapy

  2025cites this paper
• Thiazole conjugated amino acid derivatives as potent cytotoxic agents

  2025cites this paper
• Exploring the synthetic developments and pharmacological potential of 2-amino/hydrazino-4-arylthiazoles: a review

  2025cites this paper
• Identification of potential Abl kinase inhibitors using virtual screening and free energy calculations for the treatment of chronic myeloid leukemia.

  2025cites this paper
• Senescent brain cell types in Alzheimer's disease: Pathological mechanisms and therapeutic opportunities

  2025cites this paper
• Dasatinib inhibits PD-L1 expression via a proteasomal pathway in pancreatic ductal adenocarcinoma cells

  2025cites this paper
• Cardiovascular Disease in Patients With Chronic Myeloid Leukemia

  2025cites this paper
• Drug Interaction of Dasatinib with Thymoquinone: A Pharmacokinetic Study in Rats

  2025cites this paper
• Dearomative Difluoromethylation of N-Heterocycles and Pharmaceuticals with Bromo(difluoro)acetic Acid.

  2025cites this paper
• Dual Inhibition of SRC Family Kinases and Sorafenib Enhances Anti-Tumor Activity in Hepatocellular Carcinoma Cells

  2025cites this paper
• SRC at the Crossroads of KRAS Inhibitor Resistance: Mechanisms and Therapeutic Opportunities.

  2025cites this paper
• Targeting DNA damage in ageing: towards supercharging DNA repair

  2025cites this paper
• Bacterial ubiquitin ligase engineered for small molecule and protein target identification

  2025cites this paper
• Prognostic significance and potential association between ALDOA and ENO1 in gastric cancer

  2025cites this paper
• Single-cell morphological tracking of cell states to identify small-molecule modulators of liver differentiation

  2025cites this paper
• Piezo1-mediated mechanotransduction controls osteocyte maturation and dendrite development via a YAP-CCN-Src signaling axis

  2025cites this paper
• LCK at the Crossroad of Immunodeficiency and Autoimmunity: Mechanisms and Therapeutic Opportunities.

  2025cites this paper
• Chemical Adaptation in Drug Discovery: The Medicinal Chemistry Journey of Olverembatinib and Limertinib in Overcoming Kinase Drug Resistance.

  2025cites this paper
• Post-Translational Modifications Remodel Proteome-Wide Ligandability

  2025cites this paper
• KIT-Mutant Melanoma: Understanding the Pathway to Personalized Therapy

  2025cites this paper
• Functional, Pharmacogenomic, and Immune Landscapes of Long Non‐Coding RNAs in Cancer

  2025cites this paper
• Identification of N-tert-butyloxycarbonyl protected amino acids as novel hydrophobic tags to induce targeted protein degradation.

  2025cites this paper
• Optimizing Adamantane Derivatives for Enhanced EGFR Inhibition in MCF-7 Breast Cancer Cells

  2025cites this paper
• Structure-based identification of Jervine as a potent dual-targeting inhibitor of cell cycle kinases

  2025cites this paper
• Tempered signal strength via low-dose MEK inhibition optimizes therapeutic performance of engineered T cells

  2025cites this paper
• Characterization of Protein-Ligand Chalcogen Bonds: Insights from Database Survey and Quantum Mechanics Calculations

  2025cites this paper
• Systematic identification of cancer pathways and potential drugs for intervention through multi-omics analysis

  2025cites this paper
• A human neuron Alzheimer’s disease model reveals barriers to senolytic translatability

  2025cites this paper
• Imatinib and blinatumomab successfully rescued a pediatric B-ALL patient with TERF2::PDGFRB fusion resistant to dasatinib and chemotherapy

  2025cites this paper
• Protein Kinase Inhibitors: Synthesis and Molecular Repurposing in Three‐Dimensional Cancer Models PKI

  2025cites this paper
• Autophosphorylation of oncoprotein TEL-ABL in myeloid and lymphoid cells confers resistance to the allosteric ABL inhibitor asciminib.

  2025cites this paper
• Ponatinib: A Review of the History of Medicinal Chemistry behind Its Development

  2024cites this paper
• Integrin signaling in pluripotent cells acts as a gatekeeper of mouse germline entry

  2024cites this paper
• Mutations in Ras homolog family member A in patients with peripheral T-cell lymphoma and implications for personalized medicine

  2024cites this paper
• Significance of Somatic Mutation Profiling in CML Beyond BCR-ABL: A Retrospective Study of the Indian Population

  2024cites this paper
• Grb2 Phosphorylation Antagonizes EGFR-driven Ras Activation by Interfering with Condensate Assembly

  2024cites this paper
• Chronic myeloid leukemia: 2025 update on diagnosis, therapy, and monitoring

  2024cites this paper
• Thiazole‐Based IL‐17 Inhibitors Discovered by Scaffold Morphing

  2024cites this paper
• Pyridine-mediated efficient synthesis of (benzo)thiazoles-containing amides via the acylation of 2‐amino(benzo)thiazoles under ultrasonic irradiation

  2024cites this paper
• 4-Methylthiazole triggers apoptosis and mitochondrial disruption in HL-60 cells

  2024cites this paper
• Synthesis and biological characterisation of a des-aza-dasatinib tool compound

  2024cites this paper
• Dasatinib loaded mucoadhesive lecithin-chitosan hybrid nanoparticles for its augmented oral delivery, in-vitro efficacy and safety.

  2024cites this paper
• The intrinsic substrate specificity of the human tyrosine kinome

  2024cites this paper
• Design and Synthesis of Metalloporphyrin Nanoconjugates for Dual Light-Responsive Antimicrobial Photodynamic Therapy.

  2024cites this paper
• Tyrosine kinase inhibitor response of ABL-class acute lymphoblastic leukemia: the role of kinase type and SH3 domain

  2024cites this paper
• Dasatinib induces endothelial dysfunction leading to impaired recovery from ischaemia

  2024cites this paper
• Estimation of Ligand Binding Free Energy Using Multi-eGO

  2024cites this paper
• Structural elucidation, Hirshfeld surface, DFT, molecular docking and molecular dynamics studies of a novel thiazole derivative as anti-cancer drug

  2024cites this paper
• FDA-approved small molecule kinase inhibitors for cancer treatment (2001-2015): Medical indication, structural optimization, and binding mode Part I.

  2024cites this paper
• Imatinib decreases germ cell survival and germline stem cell proliferation in rodent testis ex vivo and in vitro

  2024cites this paper
• Molecular Pharmacology of Dasatinib Provides Unique Insights into the Mechanistic Basis of Success and Failure of Targeted Cancer Therapy.

  2024cites this paper
• Antitumor effects of inhibitors of ERK and Akt pathways in canine histiocytic sarcoma cell lines.

  2024cites this paper
• Halloysite Nanotube-Based Delivery of Pyrazolo[3,4-d]pyrimidine Derivatives for Prostate and Bladder Cancer Treatment

  2024cites this paper
• Structure Optimization, Synthesis and Bioactivity Evaluation of Novel BCR-ABL Tyrosine Kinase Inhibitor Targeting T315I Mutation.

  2024cites this paper
• A comprehensive update on the potential of curcumin to enhance chemosensitivity in colorectal cancer

  2024cites this paper
• Synthesis and Evaluation of Thiazolyl-indole-2-carboxamide Derivatives as Potent Multitarget Anticancer Agents

  2024cites this paper
• DCAF1-based PROTACs with activity against clinically validated targets overcoming intrinsic- and acquired-degrader resistance

  2024cites this paper
• Recurrent Herpes Infection in Two Cases with Chronic Myeloid Leukemia Using Dasatinib

  2023cites this paper
• Mechanosensing via a GpIIb/Src/14-3-3ζ axis critically regulates platelet migration in vascular inflammation

  2023cites this paper
• Reinstating targeted protein degradation with DCAF1 PROTACs in CRBN PROTAC resistant settings

  2023cites this paper
• Design, Synthesis, and anticancer evaluation of new 1-allyl-4-oxo-6-(3,4,5-trimethoxyphenyl)-1,4-dihydropyrimidine-5-carbonitrile bearing pyrazole moieties.

  2023cites this paper
• Adverse Toxic Effects of Tyrosine Kinase Inhibitors on Non-Target Zebrafish Liver (ZFL) Cells

  2023cites this paper
• Differential Chemoproteomics Reveals MARK2/3 as Cell Migration‐Relevant Targets of the ALK Inhibitor Brigatinib

  2023cites this paper
• Synthesis of SNIPERs against BCR-ABL with kinase inhibitors and a method to evaluate their growth inhibitory activity derived from BCR-ABL degradation.

  2023cites this paper
• A Novel Gemcitabine-Resistant Gallbladder Cancer Model Provides Insights into Molecular Changes Occurring during Acquired Resistance

  2023influential citation
• Application and synthesis of thiazole ring in clinically approved drugs.

  2023cites this paper
• Glypican‐4 regulated actin cytoskeletal reorganization in glucocorticoid treated trabecular meshwork cells and involvement of Wnt/PCP signaling

  2023cites this paper
• Insights on hematopoietic cell kinase: An oncogenic player in human cancer.

  2023cites this paper
• Pharmacokinetics and safety of dasatinib and its generic: a phase I bioequivalence study in healthy Chinese subjects

  2023influential citation
• High-throughput screen in vitro identifies dasatinib as a candidate for combinatorial treatment with HER2-targeting drugs in breast cancer

  2023cites this paper
• Bosutinib Stimulates Macrophage Survival, Phagocytosis, and Intracellular Killing of Bacteria

  2023cites this paper
• Comparative Analysis of Dasatinib Effect between 2D and 3D Tumor Cell Cultures

  2023cites this paper
• Bioinformatics Analysis of the Prognostic Significance of VPS16 in Hepatocellular Carcinoma and Its Role in Drug Screening

  2023cites this paper
• Differential inhibition of T-cell receptor and STAT5 signaling pathways determines the immunomodulatory effects of dasatinib in chronic phase chronic myeloid leukemia

  2023cites this paper
• The oncogenic roles and clinical implications of YAP/TAZ in breast cancer

  2023cites this paper
• Harmonizing the Craft of Crafting Clinically Endorsed Small-Molecule BCR-ABL Tyrosine Kinase Inhibitors for the Treatment of Hematological Malignancies.

  2023cites this paper
• Atypical N-Alkyl to N-Noralkoxy Switch in a Dual cSRC/BCR-ABL1 Kinase Inhibitor Improves Drug Efflux and hERG Affinity

  2023cites this paper
• Pharmacological Targeting of Senescence with Senolytics as a New Therapeutic Strategy for Neurodegeneration

  2023cites this paper
• A synergistic investigation of azo-thiazole derivatives incorporating thiazole moieties: a comprehensive exploration of their synthesis, characterization, computational insights, solvatochromism, and multimodal biological activity assessment

  2023cites this paper
• Selective and Potent PROTAC Degraders of c-Src Kinase.

  2023cites this paper
• Transporter-Mediated Cellular Distribution of Tyrosine Kinase Inhibitors as a Potential Resistance Mechanism in Chronic Myeloid Leukemia

  2023cites this paper
• Molecular pathogenesis, mechanism and therapy of Cav1 in prostate cancer

  2023cites this paper
• Increased c‑SRC expression is involved in acquired resistance to lenvatinib in hepatocellular carcinoma

  2023influential citation
• Single-cell morphological tracking of liver cell states to identify small-molecule modulators of liver differentiation

  2023cites this paper
• The Progress of Small Molecule Targeting BCR-ABL in the Treatment of Chronic Myeloid Leukemia.

  2023cites this paper
• Antibody drug conjugates beyond cytotoxic payloads.

  2023cites this paper
• Recent advances of small-molecule c-Src inhibitors for potential therapeutic utilities.

  2023cites this paper
• Recent drug design strategies and identification of key heterocyclic scaffolds for promising anticancer targets.

  2023cites this paper