4.7 Article

Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors

Related references

Note: Only part of the references are listed.
Article Biochemistry & Molecular Biology

Evaluation of imidazo[2,1-b]thiazole-based anticancer agents in one decade (2011-2020): Current status and future prospects

Rawan M. Sbenati et al.

Summary: This article reviewed the potential anticancer properties of imidazo[2,1-b]thiazole derivatives, focusing on their biological characteristics and structure-activity relationship (SAR). Reports published in the literature from 2011 to 2020 were the main focus of this review.

BIOORGANIC & MEDICINAL CHEMISTRY (2021)

Article Chemistry, Medicinal

Design, synthesis, biological evaluation, and modeling studies of novel conformationally-restricted analogues of sorafenib as selective kinase-inhibitory antiproliferative agents against hepatocellular carcinoma cells

Rawan M. Sbenati et al.

Summary: Novel indole-based rigid analogues of sorafenib were designed and synthesized to enhance kinase selectivity, with compound 1h showing superior antiproliferative potency against HCC cell lines compared to sorafenib. Compound 1h exhibited promising selectivity against HCC cells, superior kinase selectivity to sorafenib, and the ability to inhibit VEGFR2 kinase dose-dependently within Hep-G2 HCC cells.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Medicinal

Discovery of New Imidazo[2,1-b]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising In Vitro and In Vivo Anti-melanoma Activity

Mohammed S. Abdel-Maksoud et al.

Summary: In this study, a series of new (imidazo[2,1-b]thiazol-5-yl)pyrimidine derivatives with a terminal sulfonamide moiety were synthesized and their pan-RAF inhibitory effect was investigated. Compounds 27c and 38a showed the highest antiproliferative activity against cancer cells and were able to inhibit phosphorylation of MEK and ERK. Compound 38a was further tested for its in vivo activity against melanoma, and both cellular and animal activities were reported.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Review Oncology

The role of ErbB4 in cancer

Vincent F. M. Segers et al.

CELLULAR ONCOLOGY (2020)

Article Biochemistry & Molecular Biology

Imidazothiazole-based potent inhibitors of V600E-B-RAF kinase with promising anti-melanoma activity: biological and computational studies

Hanan S. Anbar et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2020)

Review Chemistry, Medicinal

Clinical evaluation of dacomitinib for the treatment of metastatic non-small cell lung cancer (NSCLC): current perspectives

Daniele Lavacchi et al.

DRUG DESIGN DEVELOPMENT AND THERAPY (2019)

Article Biochemistry & Molecular Biology

Discovery of highly potent V600E-B-RAF kinase inhibitors: Molecular modeling study

Hamadeh Tarazi et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2019)

Article Biochemistry & Molecular Biology

Ibrutinib inhibition of ERBB4 reduces cell growth in a WNT5A-dependent manner

Femina Rauf et al.

ONCOGENE (2018)

Review Oncology

Neratinib, A Novel HER2-Targeted Tyrosine Kinase Inhibitor

Shruti Rakesh Tiwari et al.

CLINICAL BREAST CANCER (2016)

Article Oncology

ERBB4 is over-expressed in human colon cancer and enhances cellular transformation

Christopher S. Williams et al.

CARCINOGENESIS (2015)

Article Chemistry, Medicinal

Design, synthesis, in vitro antiproliferative evaluation, and kinase inhibitory effects of a new series of imidazo[2,1-b]thiazole derivatives

Mohammed S. Abdel-Maksoud et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2015)

Article Oncology

Convergent and Divergent Cellular Responses by ErbB4 Isoforms in Mammary Epithelial Cells

Vikram B. Wali et al.

MOLECULAR CANCER RESEARCH (2014)

Review Pharmacology & Pharmacy

A comprehensive review of the preclinical efficacy profile of the ErbB family blocker afatinib in cancer

Helmout Modjtahedi et al.

NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY (2014)

Article Chemistry, Medicinal

New imidazo[2,1-b]thiazole derivatives: Synthesis, in vitro anticancer evaluation, and in silico studies

Jin-Hun Park et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2011)

Article Pharmacology & Pharmacy

Mechanism of cytochrome P450-3A inhibition by ketoconazole

David J. Greenblatt et al.

JOURNAL OF PHARMACY AND PHARMACOLOGY (2011)

Review Biochemistry & Molecular Biology

Catalytic Control in the EGF Receptor and Its Connection to General Kinase Regulatory Mechanisms

Natalia Jura et al.

MOLECULAR CELL (2011)

Article Oncology

ERBB3/HER3 and ERBB2/HER2 duet in mammary development and breast cancer

David F. Stern

JOURNAL OF MAMMARY GLAND BIOLOGY AND NEOPLASIA (2008)

Article Cell Biology

TheEGF receptor family: spearheading a merger of signaling and therapeutics

Erez M. Bublil et al.

CURRENT OPINION IN CELL BIOLOGY (2007)

Article Oncology

The role of HER1-HER4 and EGFRvIII in hormone-refractory prostate cancer

J Edwards et al.

CLINICAL CANCER RESEARCH (2006)

Review Pharmacology & Pharmacy

Small molecules with EGFR-TK inhibitor activity

J Albanell et al.

CURRENT DRUG TARGETS (2005)

Article Biochemical Research Methods

IonWorks™ HT:: A new high-throughput electrophysiology measurement platform

K Schroeder et al.

JOURNAL OF BIOMOLECULAR SCREENING (2003)

Review Biochemistry & Molecular Biology

ST1571 (Gleevec (TM)) as a paradigm for cancer therapy

BJ Druker

TRENDS IN MOLECULAR MEDICINE (2002)