Antitumor activity and mechanisms of dual EGFR/DNA-targeting strategy for the treatment of lung cancer with EGFRL858R/T790M mutation.

[1]  Y. Liu,et al.  Novel nitrogen mustard-artemisinin hybrids with potent anti-leukemia action through DNA damage and activation of GPx. , 2022, European journal of medicinal chemistry.

[2]  Tao Zhang,et al.  Conformational Constrained 4-(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations. , 2022, Journal of medicinal chemistry.

[3]  S. Misale,et al.  Resistance is futile with fourth-generation EGFR inhibitors , 2022, Nature Cancer.

[4]  Yongyi Mao,et al.  Discovery of Potent PROTACs Targeting EGFR Mutants through the Optimization of Covalent EGFR Ligands. , 2022, Journal of medicinal chemistry.

[5]  Lin-jiang Tong,et al.  Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors. , 2022, European journal of medicinal chemistry.

[6]  Ri-zhen Huang,et al.  (±)-Corysaxicolaine A: a pair of antitumor enantiomeric alkaloid dimers from Corydalis saxicola. , 2022, Organic & biomolecular chemistry.

[7]  Dahong Li,et al.  Design and synthesis of chromone-nitrogen mustard derivatives and evaluation of anti-breast cancer activity , 2021, Journal of enzyme inhibition and medicinal chemistry.

[8]  C. Xie,et al.  Mechanisms and management of 3rd-generation EGFR-TKI resistance in advanced non-small cell lung cancer (Review) , 2021, International journal of oncology.

[9]  T. Mitsudomi,et al.  Drug Tolerance to EGFR Tyrosine Kinase Inhibitors in Lung Cancers with EGFR Mutations , 2021, Cells.

[10]  Bin Zhang,et al.  Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors. , 2021, European journal of medicinal chemistry.

[11]  Kahksha,et al.  Novel quinazoline-based EGFR kinase inhibitors: A review focussing on SAR and molecular docking studies (2015-2019). , 2020, European journal of medicinal chemistry.

[12]  Yanmin Zhang,et al.  Discovery of coumarin derivatives as potent and selective cyclin-dependent kinase 9 (CDK9) inhibitors with high antitumour activity. , 2020, European journal of medicinal chemistry.

[13]  Wen-en Zhao,et al.  Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFRL858R/T790M NSCLCs by the conformation constrained strategy. , 2020, European journal of medicinal chemistry.

[14]  A. Gemma,et al.  Gefitinib Alone Versus Gefitinib Plus Chemotherapy for Non-Small-Cell Lung Cancer With Mutated Epidermal Growth Factor Receptor: NEJ009 Study. , 2020, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[15]  Bing Xu,et al.  Synthetic Lethality of Combined AT-101 with Idarubicin in Acute Myeloid Leukemia via Blockade of DNA Repair and Activation of Intrinsic Apoptotic Pathway. , 2019, Cancer letters.

[16]  Bin Zhang,et al.  Promoting antitumor efficacy by suppressing hypoxia via nano self-assembly of two irinotecan-based dual drug conjugates having a HIF-1α inhibitor. , 2019, Journal of materials chemistry. B.

[17]  Yi-long Wu,et al.  Clinical management of third-generation EGFR inhibitor-resistant patients with advanced non-small cell lung cancer: Current status and future perspectives. , 2019, Cancer letters.

[18]  Benjamin P. Brown,et al.  On-target Resistance to the Mutant-Selective EGFR Inhibitor Osimertinib Can Develop in an Allele-Specific Manner Dependent on the Original EGFR-Activating Mutation , 2019, Clinical Cancer Research.

[19]  Luqing Zhao,et al.  Design and Evaluation of Potent EGFR Inhibitors through the Incorporation of Macrocyclic Polyamine Moieties into the 4-Anilinoquinazoline Scaffold. , 2018, Journal of medicinal chemistry.

[20]  G. O’Kane,et al.  Resistance to epidermal growth factor receptor tyrosine kinase inhibitors, T790M, and clinical trials. , 2018, Current oncology.

[21]  Christina H. Stuelten,et al.  Cell motility in cancer invasion and metastasis: insights from simple model organisms , 2018, Nature Reviews Cancer.

[22]  Huabei Zhang,et al.  Design and synthesis of novel pyrazolo[1,5-a]pyrimidine derivatives bearing nitrogen mustard moiety and evaluation of their antitumor activity in vitro and in vivo. , 2016, European journal of medicinal chemistry.

[23]  Haikuo Zhang,et al.  Overcoming EGFR T790M and C797S resistance with mutant-selective allosteric inhibitors , 2016 .

[24]  Wei Huang,et al.  A chemical tuned strategy to develop novel irreversible EGFR-TK inhibitors with improved safety and pharmacokinetic profiles. , 2014, Journal of medicinal chemistry.

[25]  J. Bajorath,et al.  Polypharmacology: challenges and opportunities in drug discovery. , 2014, Journal of medicinal chemistry.

[26]  Wenbing Chen,et al.  Aromatic nitrogen mustard-based prodrugs: activity, selectivity, and the mechanism of DNA cross-linking. , 2014, Chemistry.

[27]  Juswinder Singh,et al.  Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC. , 2013, Cancer discovery.

[28]  Matthew Grist,et al.  Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR). , 2013, Journal of medicinal chemistry.

[29]  D. Lauffenburger,et al.  Targeting tumor cell motility as a strategy against invasion and metastasis. , 2013, Trends in pharmacological sciences.

[30]  Yoshikazu Ohta,et al.  Structure-Based Approach for the Discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors. , 2013, ACS medicinal chemistry letters.

[31]  Xiang Yan,et al.  Chlorambucil for patients with primary biliary cirrhosis. , 2012, The Cochrane database of systematic reviews.

[32]  Z. Ge,et al.  Novel EGFR inhibitors prepared by combination of dithiocarbamic acid esters and 4-anilinoquinazolines. , 2011, Bioorganic & medicinal chemistry letters.

[33]  James H. Doroshow,et al.  Utilizing targeted cancer therapeutic agents in combination: novel approaches and urgent requirements , 2010, Nature Reviews Drug Discovery.

[34]  W. Hait,et al.  Anticancer drug development: the grand challenges , 2010, Nature Reviews Drug Discovery.

[35]  R. Brodsky High-dose cyclophosphamide for autoimmunity and alloimmunity , 2010, Immunologic research.

[36]  George Iliakis,et al.  γ-H2AX in recognition and signaling of DNA double-strand breaks in the context of chromatin , 2008, Nucleic acids research.

[37]  P. Jänne,et al.  Mechanisms of Acquired Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non–Small Cell Lung Cancer , 2008, Clinical Cancer Research.

[38]  Matthew Meyerson,et al.  Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity. , 2007, Cancer cell.

[39]  D. Schuppan,et al.  Erlotinib induces cell cycle arrest and apoptosis in hepatocellular cancer cells and enhances chemosensitivity towards cytostatics. , 2005, Journal of hepatology.

[40]  Penny A. Johnson,et al.  The in vitro effect of gefitinib ('Iressa') alone and in combination with cytotoxic chemotherapy on human solid tumours , 2004, BMC Cancer.

[41]  Alberto Martínez,et al.  Design, synthesis, and biological activity of hybrid compounds between uramustine and DNA minor groove binder distamycin A. , 2002, Journal of medicinal chemistry.

[42]  G. Faguet,et al.  Chronic lymphocytic leukemia: an updated review. , 1994, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[43]  A. Gilman,et al.  The biological actions and therapeutic applications of the B-chloroethyl amines and sulfides. , 1946, Science.

[44]  A. Fabbri,et al.  Myelosuppression after frontline fludarabine, cyclophosphamide, and rituximab in patients with chronic lymphocytic leukemia: Analysis of persistent and new‐onset cytopenia , 2014, Cancer.

[45]  R. Kyle,et al.  Multiple myeloma: diagnosis and treatment. , 2005, Mayo Clinic proceedings.