Novel, selective acrylamide linked quinazolines for the treatment of double mutant EGFR-L858R/T790M Non-Small-Cell lung cancer (NSCLC)

Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold

(2020) Min Sun et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

GLORYx: Prediction of the Metabolites Resulting from Phase 1 and Phase 2 Biotransformations of Xenobiotics

(2020) Christina de Bruyn Kops et al.   CHEMICAL RESEARCH IN TOXICOLOGY

The test that changed the world: The Ames test and the regulation of chemicals

(2019) Errol Zeiger   MUTATION RESEARCH-GENETIC TOXICOLOGY AND ENVIRONMENTAL MUTAGENESIS

Target Dose Versus Maximum Tolerated Dose in Heart Failure

(2019) Biykem Bozkurt   JACC-Heart Failure

Why maximum tolerated dose?

(2019) Hans G. Stampfer et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

FAME 3: Predicting the Sites of Metabolism in Synthetic Compounds and Natural Products for Phase 1 and Phase 2 Metabolic Enzymes

(2019) Martin Šícho et al.   Journal of Chemical Information and Modeling

Potent hERG channel inhibition by sarizotan, an investigative treatment for Rett Syndrome

(2019) Hongwei Cheng et al.   JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY

In-silico evidences for binding of Glucokinase activators to EGFR C797S to overcome EGFR resistance obstacle with mutant-selective allosteric inhibition

(2018) Harun Patel et al.   COMPUTATIONAL BIOLOGY AND CHEMISTRY

Derivation of avian dermal LD50 values for dermal exposure models using in vitro percutaneous absorption of [ 14 C]-atrazine through rat, mallard, and northern bobwhite full thickness skin

(2018) Jonathan D. Maul et al.   SCIENCE OF THE TOTAL ENVIRONMENT

Resolving the Mystery of Ring Opening in the Synthesis of benzo[d][1,3]oxazin-4-one and quinazolin-4(3H)-one

(2018) Harun Patel et al.   LETTERS IN ORGANIC CHEMISTRY

Structural and functional aspects of P-glycoprotein and its inhibitors

(2018) Shirin Mollazadeh et al.   LIFE SCIENCES

Design, synthesis and biological evaluation of AZD9291 derivatives as selective and potent EGFRL858R/T790M inhibitors

(2018) Bingbing Zhao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance

(2017) Harun Patel et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Epidermal Growth Factor Receptor Cell Proliferation Signaling Pathways

(2017) et al.   Cancers

The micro-Ames test: A direct comparison of the performance and sensitivities of the standard and 24-well plate versions of the bacterial mutation test

(2016) Raymond Proudlock et al.   ENVIRONMENTAL AND MOLECULAR MUTAGENESIS

Challenges and Perspectives on the Development of Small-Molecule EGFR Inhibitors against T790M-Mediated Resistance in Non-Small-Cell Lung Cancer

(2016) Zhendong Song et al.   JOURNAL OF MEDICINAL CHEMISTRY

Anti-convulsant potential of quinazolinones

(2016) Harun M. Patel et al.   RSC Advances

Epidermal Growth Factor Receptor (EGFR) Tyrosine Kinase Inhibitors from the Natural Origin: A Recent Perspective

(2015) Harun Patel et al.   Anti-Cancer Agents in Medicinal Chemistry

Volume of Distribution in Drug Design

(2015) Dennis A. Smith et al.   JOURNAL OF MEDICINAL CHEMISTRY

pkCSM: Predicting Small-Molecule Pharmacokinetic and Toxicity Properties Using Graph-Based Signatures

(2015) Douglas E. V. Pires et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure-Based Virtual Screening Approach for Discovery of Covalently Bound Ligands

(2014) Dora Toledo Warshaviak et al.   Journal of Chemical Information and Modeling

Docking Covalent Inhibitors: A Parameter Free Approach To Pose Prediction and Scoring

(2014) Kai Zhu et al.   Journal of Chemical Information and Modeling

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

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

Design, synthesis and in vitro anti-proliferative activity of 4,6-quinazolinediamines as potent EGFR-TK inhibitors

(2012) Samar Mowafy et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Randomized Phase II Study of Dacomitinib (PF-00299804), an Irreversible Pan–Human Epidermal Growth Factor Receptor Inhibitor, Versus Erlotinib in Patients With Advanced Non–Small-Cell Lung Cancer

(2012) Suresh S. Ramalingam et al.   JOURNAL OF CLINICAL ONCOLOGY

CovalentDock: Automated covalent docking with parameterized covalent linkage energy estimation and molecular geometry constraints

(2012) Xuchang Ouyang et al.   JOURNAL OF COMPUTATIONAL CHEMISTRY

Non-Small Cell Lung Cancer: Epidemiology, Risk Factors, Treatment, and Survivorship

(2012) Julian R. Molina et al.   MAYO CLINIC PROCEEDINGS

The EGFR T790M Mutation in Acquired Resistance to an Irreversible Second-Generation EGFR Inhibitor

(2012) Y. Kim et al.   MOLECULAR CANCER THERAPEUTICS

Phase I study of continuous afatinib (BIBW 2992) in patients with advanced non-small cell lung cancer after prior chemotherapy/erlotinib/gefitinib (LUX-Lung 4)

(2011) H. Murakami et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Drug-permeability and transporter assays in Caco-2 and MDCK cell lines

(2011) Donna A Volpe   Future Medicinal Chemistry

Synthesis, method optimization, anticancer activity of 2,3,7-trisubstituted Quinazoline derivatives and targeting EGFR-tyrosine kinase by rational approach

(2011) Malleshappa N. Noolvi et al.   Arabian Journal of Chemistry

Chronic oral LOAEL prediction by using a commercially available computational QSAR tool

(2010) Bernd Rupp et al.   ARCHIVES OF TOXICOLOGY

Chemogenomic Profiling Provides Insights into the Limited Activity of Irreversible EGFR Inhibitors in Tumor Cells Expressing the T790M EGFR Resistance Mutation

(2010) M. L. Sos et al.   CANCER RESEARCH

Molecular Diagnosis of Activating EGFR Mutations in Non-Small Cell Lung Cancer Using Mutation-Specific Antibodies for Immunohistochemical Analysis

(2010) A. Kawahara et al.   CLINICAL CANCER RESEARCH

Targeted covalent drugs of the kinase family

(2010) Juswinder Singh et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

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

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

AutoDock4 and AutoDockTools4: Automated docking with selective receptor flexibility

(2009) Garrett M. Morris et al.   JOURNAL OF COMPUTATIONAL CHEMISTRY

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

(2009) Wenjun Zhou et al.   NATURE

Drugs Behave as Substrates, Inhibitors and Inducers of Human Cytochrome P450 3A4

(2008) Shu-Feng Zhou   CURRENT DRUG METABOLISM

EGFR Mutations in Lung Adenocarcinomas

(2008) Allan R. Li et al.   JOURNAL OF MOLECULAR DIAGNOSTICS

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