Structure activity relationships of chrysoeriol and analogs as dual c‑Met and VEGFR2 tyrosine kinase inhibitors
نویسندگان
چکیده
منابع مشابه
Myeloproliferative Neoplasms Associated with Mutation in JAK2V617F and Tyrosine Kinase Inhibitors as Therapeutic Strategy
MPNs including a heterogeneous group of clonal or oligoclonal hamtopathies characterized by proliferation and accumulation of mature myeloid cells. JAK2 tyrosine kinase mutation is the most common molecular lesion identified in 90% of cases. JAK2 is involved in EPO signaling pathway, and mutations in it lead to EPO-independent spontaneous phosphorylation. Most tyrosine kinase inhibitors (TKI) a...
متن کاملStructure–Activity Relationships and Molecular Modeling of Sphingosine Kinase Inhibitors
The design, synthesis, and evaluation of the potency of new isoform-selective inhibitors of sphingosine kinases 1 and 2 (SK1 and SK2), the enzyme that catalyzes the phosphorylation of d-erythro-sphingosine to produce the key signaling lipid, sphingosine 1-phosphate, are described. Recently, we reported that 1-(4-octylphenethyl)piperidin-4-ol (RB-005) is a selective inhibitor of SK1. Here we rep...
متن کاملStructure-activity relationships of synthetic analogs of (-)-epigallocatechin-3-gallate as proteasome inhibitors.
BACKGROUND Cancer-related molecular targets of green tea polyphenols, such as (-)-epigallocatechin-3-gallate [(-)-EGCG], remain unknown. We previously showed that (-)-EGCG is a potent and specific inhibitor of the proteasomal chymotrypsin-like activity in vitro and in vivo. MATERIALS AND METHODS EGCG amides and five simple analogs were prepared by enantioselective synthesis. Proteasome inhibi...
متن کامل2D-QSAR and docking studies of 4-anilinoquinazoline derivatives as epidermal growth factor receptor tyrosine kinase inhibitors
Introduction: Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor derivatives play an important role in the treatment of cancer. We aim to construct 2D-QSAR models using various chemometrics using 4-anilinoquinazoline-containing EGFR TKIs. In addition, the binding profile of these compounds was evaluated using a docking study. Materials and Methods: In this study, 122 compounds of...
متن کاملStructure–Activity Relationship Studies with Tetrahydroquinoline Analogs as EPAC Inhibitors
EPAC proteins are therapeutic targets for the potential treatment of cardiac hypertrophy and cancer metastasis. Several laboratories use a tetrahydroquinoline analog, CE3F4, to dissect the role of EPAC1 in various disease states. Here, we report SAR studies with tetrahydroquinoline analogs that explore various functional groups. The most potent EPAC inhibitor 12a exists as a mixture of insepara...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Oncology Reports
سال: 2018
ISSN: 1021-335X,1791-2431
DOI: 10.3892/or.2018.6542