A new series of antileukemic agents: Design, synthesis, in vitro and in silico evaluation of thiazole-based ABL1 kinase inhibitors
E Zeytün, MD Altıntop, B Sever… - Anti-Cancer Agents …, 2021 - ingentaconnect.com
Background: After the approval of imatinib, more than 25 antitumor agents targeting kinases
have been approved, and several promising candidates are at various stages of clinical …
have been approved, and several promising candidates are at various stages of clinical …
Design, synthesis, and biological evaluation of novel 1, 3, 4-thiadiazole derivatives as potential antitumor agents against chronic myelogenous leukemia: Striking …
In an attempt to develop potent antitumor agents, new 1, 3, 4-thiadiazole derivatives were
synthesized and evaluated for their cytotoxic effects on multiple human cancer cell lines …
synthesized and evaluated for their cytotoxic effects on multiple human cancer cell lines …
Design, synthesis, and biological evaluations of novel 3-amino-4-ethynyl indazole derivatives as Bcr-Abl kinase inhibitors with potent cellular antileukemic activity
AK El-Damasy, H Jin, SH Seo, EK Bang… - European Journal of …, 2020 - Elsevier
Abstract Breakpoint cluster region-Abelson (Bcr-Abl) kinase is a key driver in the
pathophysiology of chronic myelogenous leukemia (CML). Broadening the chemical …
pathophysiology of chronic myelogenous leukemia (CML). Broadening the chemical …
[HTML][HTML] Structural optimization of 4-(imidazol-5-yl) pyridine derivatives affords broad-spectrum anticancer agents with selective B-RAFV600E/p38α kinase inhibitory …
In the current article, we introduce design of a new series of 4-(imidazol-5-yl) pyridines with
improved anticancer activity and selective B-RAF V600E/p38α kinase inhibitory activity …
improved anticancer activity and selective B-RAF V600E/p38α kinase inhibitory activity …
Discovery and SAR of 1, 3, 4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents
A series of substituted benzoylamino-2-[(4-benzyl) thio]-1, 3, 4-thiadiazoles has been
discovered as potent Abl tyrosine kinase inhibitors. Molecular docking simulations on the …
discovered as potent Abl tyrosine kinase inhibitors. Molecular docking simulations on the …
Novel guanidine derivatives targeting leukemia as selective Src/Abl dual inhibitors: Design, synthesis and anti-proliferative activity
A new series of benzene-sulfonamide derivatives 3a-i was designed and synthesized via
the reaction of N-(pyrimidin-2-yl) cyanamides 1a-i with sulfamethazine sodium salt 2 as dual …
the reaction of N-(pyrimidin-2-yl) cyanamides 1a-i with sulfamethazine sodium salt 2 as dual …
Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class
E Salah, E Ugochukwu, AJ Barr… - Journal of medicinal …, 2011 - ACS Publications
ABL2 (also known as ARG (ABL related gene)) is closely related to the well-studied Abelson
kinase cABL. ABL2 is involved in human neoplastic diseases and is deregulated in solid …
kinase cABL. ABL2 is involved in human neoplastic diseases and is deregulated in solid …
[HTML][HTML] Rational drug design of Axl tyrosine kinase type I inhibitors as promising candidates against cancer
E Sarukhanyan, S Shityakov, T Dandekar - Frontiers in Chemistry, 2020 - frontiersin.org
The high level of Axl tyrosine kinase expression in various cancer cell lines makes it an
attractive target for the development of anti-cancer drugs. In this study, we carried out …
attractive target for the development of anti-cancer drugs. In this study, we carried out …
ABL kinase inhibitory and antiproliferative activity of novel picolinamide based benzothiazoles
AK El-Damasy, NC Cho, SB Kang, AN Pae… - Bioorganic & Medicinal …, 2015 - Elsevier
A series of novel picolinamide based benzothiazoles (17 final compounds), targeting both
wild-type and the most resistant T315I mutant of Bcr-Abl kinase, has been designed and …
wild-type and the most resistant T315I mutant of Bcr-Abl kinase, has been designed and …
Alkynylnicotinamide‐Based Compounds as ABL1 Inhibitors with Potent Activities against Drug‐Resistant CML Harboring ABL1 (T315I) Mutant Kinase
EA Larocque, N Naganna, C Opoku‐Temeng… - …, 2018 - Wiley Online Library
The introduction of imatinib into the clinical scene revolutionized the treatment of chronic
myelogenous leukemia (CML). The overall eight‐year survival rate for CML has increased …
myelogenous leukemia (CML). The overall eight‐year survival rate for CML has increased …