Discovery of novel thiazolyl-pyrazolines as dual EGFR and VEGFR-2 inhibitors endowed with in vitro antitumor activity towards non-small lung cancer

Discovery of new nicotinamides as apoptotic VEGFR-2 inhibitors: virtual screening, synthesis, anti-proliferative, immunomodulatory, ADMET, toxicity, and molecular dynamic simulation studies

(2022) Reda G. Yousef et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Novel 2-(5-Aryl-4,5-Dihydropyrazol-1-yl)thiazol-4-One as EGFR Inhibitors: Synthesis, Biological Assessment and Molecular Docking Insights

(2022) Tarfah Al-Warhi et al.   Drug Design Development and Therapy

Design, synthesis, and anti-cancer evaluation of new pyrido[2,3-d]pyrimidin-4(3H)-one derivatives as potential EGFRWT and EGFRT790M inhibitors and apoptosis inducers

(2022) Heba S. A. Elzahabi et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Design and synthesis of thiazolidine-2,4-diones hybrids with 1,2-dihydroquinolones and 2-oxindoles as potential VEGFR-2 inhibitors: in-vitro anticancer evaluation and in-silico studies

(2022) Mohammed S. Taghour et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

1,3,4-Oxadiazole-naphthalene hybrids as potential VEGFR-2 inhibitors: design, synthesis, antiproliferative activity, apoptotic effect, and in silico studies

(2021) Mohamed Hagras et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Dual EGFR/VEGF pathway inhibition: a promising strategy for patients with EGFR-mutant NSCLC

(2020) Xiuning Le et al.   Journal of Thoracic Oncology

Dual EGFR/VEGFR2 inhibitors and apoptosis inducers: Synthesis and antitumor activity of novel pyrazoline derivatives

(2020) Omkulthom M. Alkamaly et al.   ARCHIV DER PHARMAZIE

Novel 2-indolinone thiazole hybrids as sunitinib analogues: Design, synthesis, and potent VEGFR-2 inhibition with potential anti-renal cancer activity

(2020) Huda K. Mahmoud et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel piperazine–chalcone hybrids and related pyrazoline analogues targeting VEGFR-2 kinase; design, synthesis, molecular docking studies, and anticancer evaluation

(2020) Marwa F. Ahmed et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Synthesis, Characterization, and Biological Activity of a Novel Series of Benzo[4,5]imidazo[2,1-b]thiazole Derivatives as Potential Epidermal Growth Factor Receptor Inhibitors

(2019) Xinshan Deng et al.   MOLECULES

Novel Third-Generation EGFR Tyrosine Kinase Inhibitors and Strategies to Overcome Therapeutic Resistance in Lung Cancer

(2019) Ayesha Murtuza et al.   CANCER RESEARCH

Synthesis, anticancer effect and molecular modeling of new thiazolylpyrazolyl coumarin derivatives targeting VEGFR-2 kinase and inducing cell cycle arrest and apoptosis

(2019) Tahia K. Mohamed et al.   BIOORGANIC CHEMISTRY

Synthesis and in vitro anticancer evaluation of some fused indazoles, quinazolines and quinolines as potential EGFR inhibitors

(2019) Esraa A. Abdelsalam et al.   BIOORGANIC CHEMISTRY

Clinical management of third-generation EGFR inhibitor-resistant patients with advanced non-small cell lung cancer: Current status and future perspectives

(2019) Yi-Chen Zhang et al.   CANCER LETTERS

Synthesis, antitumour and antioxidant activities of novel α,β-unsaturated ketones and related heterocyclic analogues: EGFR inhibition and molecular modelling study

(2018) Walaa M. El-Husseiny et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Third generation EGFR TKIs: current data and future directions

(2018) Chee-Seng Tan et al.   Molecular Cancer

Receptor tyrosine kinases and downstream pathways as druggable targets for cancer treatment: the current arsenal of inhibitors

(2018) Wagner Ricardo Montor et al.   Molecular Cancer

1,3,4-oxadiazole/chalcone hybrids: Design, synthesis, and inhibition of leukemia cell growth and EGFR, Src, IL-6 and STAT3 activities

(2018) Marwa Ali A. Fathi et al.   BIOORGANIC CHEMISTRY

Synthesis and anti-proliferative activity of some new quinoline based 4,5-dihydropyrazoles and their thiazole hybrids as EGFR inhibitors

(2018) Riham F. George et al.   BIOORGANIC CHEMISTRY

Synthesis and anticonvulsant activity of some 2-pyrazolines derived from chalcones

(2017) Nagihan Beyhan et al.   Arabian Journal of Chemistry

Epidermal Growth Factor Receptor Cell Proliferation Signaling Pathways

(2017) et al.   Cancers

Identification of new potent phthalazine derivatives with VEGFR-2 and EGFR kinase inhibitory activity

(2016) Kamilia M. Amin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Covalent Modifiers: A Chemical Perspective on the Reactivity of α,β-Unsaturated Carbonyls with Thiols via Hetero-Michael Addition Reactions

(2016) Paul A. Jackson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of some new pyrazolyl-pyrazolines as potential anti-inflammatory, analgesic and antibacterial agents

(2015) Shivapura Viveka et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, biological evaluation and molecular docking of some substituted pyrazolines and isoxazolines as potential antimicrobial agents

(2015) Sameena Bano et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A novel series of thiazolyl–pyrazoline derivatives: Synthesis and evaluation of antifungal activity, cytotoxicity and genotoxicity

(2015) Mehlika Dilek Altıntop et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

DOCKTITE—A Highly Versatile Step-by-Step Workflow for Covalent Docking and Virtual Screening in the Molecular Operating Environment

(2015) Christoph Scholz et al.   Journal of Chemical Information and Modeling

Acquired EGFR C797S mutation mediates resistance to AZD9291 in non–small cell lung cancer harboring EGFR T790M

(2015) Kenneth S Thress et al.   NATURE MEDICINE

Dacomitinib in lung cancer: a “lost generation” EGFR tyrosine-kinase inhibitor from a bygone era?

(2015) Sai-Hong Ou et al.   Drug Design Development and Therapy

Acquired Resistance ofEGFR-Mutant Lung Cancer to a T790M-Specific EGFR Inhibitor

(2015) Helena A. Yu et al.   JAMA Oncology

Synthesis and biological evaluation of compounds which contain pyrazole, thiazole and naphthalene ring as antitumor agents

(2014) Ji-Wen Yuan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A phase 2 trial of dacomitinib (PF-00299804), an oral, irreversible pan-HER (human epidermal growth factor receptor) inhibitor, in patients with advanced non-small cell lung cancer after failure of prior chemotherapy and erlotinib

(2014) Karen L. Reckamp et al.   CANCER

Acquired resistance to TKIs in solid tumours: learning from lung cancer

(2014) D. Ross Camidge et al.   Nature Reviews Clinical Oncology

Non-small cell lung cancer - genetic predictors

(2013) Vladimira Koudelakova et al.   BIOMEDICAL PAPERS-OLOMOUC

Overcoming acquired resistance to anticancer therapy: focus on the PI3K/AKT/mTOR pathway

(2013) Howard A. Burris   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Novel 2-pyrazolin-1-ylthiazoles as Potential Antimicrobial Agents

(2013) Bakr Fathy Abdel-Wahab et al.   Letters in Drug Design & Discovery

Flow Cytometric Quantification of All Phases of the Cell Cycle and Apoptosis in a Two-Color Fluorescence Plot

(2013) Christine Vignon et al.   PLoS One

Bypass Mechanisms of Resistance to Receptor Tyrosine Kinase Inhibition in Lung Cancer

(2013) M. J. Niederst et al.   Science Signaling

Synthesis, molecular docking and evaluation of thiazolyl-pyrazoline derivatives containing benzodioxole as potential anticancer agents

(2012) Hai-Hong Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Facile regioselective synthesis of novel bioactive thiazolyl-pyrazoline derivatives via a three-component reaction and their antimicrobial activity

(2012) Bahman Sharifzadeh et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial

(2012) Rafael Rosell et al.   LANCET ONCOLOGY

Synthesis, molecular docking and evaluation of thiazolyl-pyrazoline derivatives as EGFR TK inhibitors and potential anticancer agents

(2011) Peng-Cheng Lv et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The therapeutic potential of targeting the EGFR family in epithelial ovarian cancer

(2011) Q Sheng et al.   BRITISH JOURNAL OF CANCER

Lung Cancer: Epidemiology, Etiology, and Prevention

(2011) Charles S. Dela Cruz et al.   CLINICS IN CHEST MEDICINE

ZD6474, a dual tyrosine kinase inhibitor of EGFR and VEGFR-2, inhibits MAPK/ERK and AKT/PI3-K and induces apoptosis in breast cancer cells

(2010) Siddik Sarkar et al.   CANCER BIOLOGY & THERAPY

New pyrazoline derivatives and their antidepressant activity

(2010) Zafer Asım Kaplancıklı et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Oncogenic mutant forms of EGFR: Lessons in signal transduction and targets for cancer therapy

(2010) Gur Pines et al.   FEBS LETTERS

Synthesis, antioxidant evaluation, and quantitative structure–activity relationship studies of chalcones

(2010) P. M. Sivakumar et al.   MEDICINAL CHEMISTRY RESEARCH

Gefitinib or Chemotherapy for Non–Small-Cell Lung Cancer with Mutated EGFR

(2010) Makoto Maemondo et al.   NEW ENGLAND JOURNAL OF MEDICINE

Combined Inhibition of the VEGFR and EGFR Signaling Pathways in the Treatment of NSCLC

(2009) N. A. Pennell et al.   ONCOLOGIST

Medicinal Chemistry and the Molecular Operating Environment (MOE): Application of QSAR and Molecular Docking to Drug Discovery

(2008) Santiago Vilar et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Evaluation of EGFR abnormalities in patients with pulmonary adenocarcinoma: the need to test neoplasms with more than one method

(2008) Ruta Gupta et al.   MODERN PATHOLOGY

BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models

(2008) D Li et al.   ONCOGENE

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

(2008) C.-H. Yun et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Combined targeting of EGFR-dependent and VEGF-dependent pathways: rationale, preclinical studies and clinical applications

(2008) Giampaolo Tortora et al.   Nature clinical practice. Oncology