Discovery of picomolar ABL kinase inhibitors equipotent for wild type and T315I mutant via structure-based de novo design
H Park, S Hong, J Kim, S Hong - Journal of the American …, 2013 - ACS Publications
Although the constitutively activated break-point cluster region–Abelson (ABL) tyrosine
kinase is known to cause chronic myelogenous leukemia (CML), the prevalence of drug …
kinase is known to cause chronic myelogenous leukemia (CML), the prevalence of drug …
[HTML][HTML] Design, synthesis, and evaluation of a new series of thiazole-based anticancer agents as potent Akt inhibitors
In an attempt to develop potent anticancer agents targeting Akt, new thiazole derivatives (1–
10) were synthesized and investigated for their cytotoxic effects on A549 human lung …
10) were synthesized and investigated for their cytotoxic effects on A549 human lung …
[HTML][HTML] New 1, 3, 4-thiadiazoles as potential anticancer agents: pro-apoptotic, cell cycle arrest, molecular modelling, and ADMET profile
A series of novel 1, 3, 4-thiadiazoles was synthesized via the reaction of N-(5-(2-
cyanoacetamido)-1, 3, 4-thiadiazol-2-yl) benzamide (3) with different carbon electrophiles …
cyanoacetamido)-1, 3, 4-thiadiazol-2-yl) benzamide (3) with different carbon electrophiles …
[HTML][HTML] Design and synthesis of novel imidazole derivatives possessing triazole pharmacophore with potent anticancer activity, and in silico ADMET with GSK-3β …
F Al-Blewi, SA Shaikh, A Naqvi, F Aljohani… - International journal of …, 2021 - mdpi.com
A library of novel imidazole-1, 2, 3-triazole hybrids were designed and synthesized based
on the hybrid pharmacophore approach. Therefore, copper (I) catalyzed click reaction of …
on the hybrid pharmacophore approach. Therefore, copper (I) catalyzed click reaction of …
In silico identification of novel kinase inhibitors targeting wild-type and T315I mutant ABL1 from FDA-approved drugs
H Xu, Z Wang, X Liang, X Li, Z Shi, N Zhou… - Molecular …, 2014 - pubs.rsc.org
The constitutively active fusion protein BCR-ABL1 is the major cause of chronic myeloid
leukemia (CML), and selective inhibition of ABL1 is a promising approach for the treatment …
leukemia (CML), and selective inhibition of ABL1 is a promising approach for the treatment …
[HTML][HTML] Design, Synthesis and Antitumor Activity of 1H-indazole-3-amine Derivatives
C Wang, M Zhu, X Long, Q Wang, Z Wang… - International Journal of …, 2023 - mdpi.com
A series of indazole derivatives were designed and synthesized by molecular hybridization
strategy, and these compounds were evaluated the inhibitory activities against human …
strategy, and these compounds were evaluated the inhibitory activities against human …
Design, synthesis and cytotoxicity evaluation of N-(5-Benzylthio)-4H-1, 2, 4-Triazol-3-YL)-4-fluorobenzamide derivatives as potential anticancer agents
A Aliabadi, A Mohammadi-Frarni, M Azizi… - Pharmaceutical …, 2016 - Springer
Despite advances in anticancer drug development and discovery, the survival of patients is
so poor. A deep need for discovery of novel anticancer drugs is among priority issues in …
so poor. A deep need for discovery of novel anticancer drugs is among priority issues in …
Synthesis of some Novel Benzimidazole derivatives as anticancer agent and evaluation for CDK2 inhibition activity
RHA El-Hameed, SS Fatahala, AI Sayed - Medicinal Chemistry, 2022 - ingentaconnect.com
Background: Thiobezimidazoles reveal various pharmacological activities due to similarities
with many natural and synthetic molecules; they can easily interact with biomolecules of …
with many natural and synthetic molecules; they can easily interact with biomolecules of …
[HTML][HTML] In vitro and in silico evaluation of antiproliferative activity of new isoxazolidine derivatives targeting EGFR: design, synthesis, cell cycle analysis, and apoptotic …
A series of novel enantiopure isoxazolidine derivatives were synthesized and evaluated for
their anticancer activities against three human cancer cell lines such as human breast …
their anticancer activities against three human cancer cell lines such as human breast …
[PDF][PDF] Exploration of anticancer potential of novel pyrrolo [2, 3-b] pyridine derivatives targeting V600E-BRAF kinase: molecular docking, pharmacokinetic and DFT …
Cancer is a type of disease that causes a threat to human health and human1life [1, 2]. In
recent years, the morbidity rate of cancer has increased [3, 4]. Cell proliferation is triggered …
recent years, the morbidity rate of cancer has increased [3, 4]. Cell proliferation is triggered …