Cover Image

Discovery of 3-((3-amino-1H-indazol-4-yl)ethynyl)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide (AKE-72), a potent Pan-BCR-ABL inhibitor including the T315I gatekeeper resistant mutant

BCR-ABL inhibition is an effective therapeutic approach for the treatment of chronic myeloid leukaemia (CML). Herein, we report the discovery of AKE-72 (5), a diarylamide 3-aminoindazole, as a potent pan-BCR-ABL inhibitor, including the imatinib-resistant mutant T315I. A focussed array of compounds...

Full description

Saved in:

Bibliographic Details
Main Authors:	Ashraf K. El-Damasy (Author), Hyun Ji Kim (Author), Jung Woo Park (Author), Yunju Nam (Author), Wooyoung Hur (Author), Eun-Kyoung Bang (Author), Gyochang Keum (Author)
Format:	Book
Published:	Taylor & Francis Group, 2023-12-01T00:00:00Z.
Subjects:	article
Online Access:	Connect to this object online.
Tags:	Add Tag No Tags, Be the first to tag this record!

Similar Items

Discovery of 4-cyclopropyl-3-(2-((1-cyclopropyl-1H-pyrazol-4-yl) amino) quinazolin-6-yl)-N-(3-(trifluoromethyl) phenyl) benzamides as potent discoidin domain receptor inhibitors for the treatment of idiopathic pulmonary fibrosis
by: Qi Wang, et al.
Published: (2022)

Synthesis, in Vivo and in Silico Studies of N-Aryl-4-(1,3-Dioxoisoindolin-2-Yl)Benzamides as an Anticonvulsant Agent
by: Parisa Kiminejad Malaie, et al.
Published: (2020)

The study of analgesic effect of 5-(furan-2-yl, 2-methylfuran-3-yl)-4-amino-1,2,4-triazole-3-thion derivatives
by: D. M. Danilchenko
Published: (2018)

Antifatigue action of the 5-(furan-2-yl, 2-metylfuran-3-yl)-4-amino-1,2,4-triazole-3-thione alkyl derivatives
by: D. M. Danilchenko, et al.
Published: (2018)

Synthesis of 2-(3-chloro-4-nitro-1-benzothien-2-yl)-1,3,4-oxadiazole-1,3,4-thiadiazole and 5-(3-chloro-4-nitro-1-benzothien-2-yl)-4H-1,2,4-triazole-3-thiol
by: Khalid M. Daoud, et al.
Published: (2010)

Design, synthesis, and anticancer evaluation of novel N-[5-(1,3,4,5-tetrahydroxycyclohexyl)-1,3,4-thiadiazole-2-yl] benzamide analogues through integrated computational and experimental approaches
by: Sujaritha Jayaraj, et al.
Published: (2024)

Synthesis, physical and chemical properties, antihypoxic activity of some 5-[((5-(adamantane-1-yl)-4-R-4H-1,2,4-triazole-3-yl)thio)methyl]-N-R1-1,3,4-thiadiazole-2-amines and 5-[((5-(adamantane-1-yl)-4-R-4H-1,2,4-triazole-3-yl)thio)methyl]-4-R1-4H-1,2,4-t
by: V. M. Odyntsova, et al.
Published: (2018)

Antimicrobial and antifungal activity of new 4-(5-((5-(alkylthio)-4-R-4H-1,2,4-triazole-3-yl)thio)-1H-1,2,4-triazole-3-yl)pyridines
by: Ye. O. Karpun, et al.
Published: (2020)

Synthesis, physical-chemical properties and further transformation of 5-(quinoline-2-yl, 2-hydroxyquinoline-4-yl)-4-R-2,4-dyhydro-3Н-1,2,4-triazole-3-thiones
by: T. M. Kaplaushenko
Published: (2016)

4-(Indol-3-yl)thiazole-2-amines and 4-ιndol-3-yl)thiazole Acylamines as Νovel Antimicrobial Agents: Synthesis, In Silico and In Vitro Evaluation
by: Sergei Simakov, et al.
Published: (2021)

Pharmacological characterization of a novel, potent, selective, and orally active fatty acid amide hydrolase inhibitor, PKM‐833 [(R)‐N‐(pyridazin‐3‐yl)‐4‐(7‐(trifluoromethyl)chroman‐4‐yl)piperazine‐1‐carboxamide] in rats: Potential for the treatment of inflammatory pain
by: Toshiya Endo, et al.
Published: (2020)

The study of the optical activity of some S-derivatives 4-R-5-((((3-(pyridin-4-yl)-1H-1,2,4-triazole-5-yl)thio)methyl)-4H-1, 2,4-triazole-3-thiols
by: Ye. O. Karpun, et al.
Published: (2022)

QSAR-analysis of 1-[2-(R-phenylimino)-4-methyl-3-(3-[morpholine-4-yl]propyl)-2,3-dihydro-1,3-thiazol-5-yl]ethane-1-one's derivatives as potential antioxidants
by: Іryna Drapak, et al.
Published: (2019)

Synthesis and properties of some 3-(5-(4-methoxyphenyl)pyrazol-3-yl)-6-R-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles
by: S. O. Fedotov, et al.
Published: (2022)

Synthesis and properties of 2-(4-phenyl-5-(((5-phenylamino-1,3,4-thiadiazole-2-yl)thio)methyl)-1,2,4-triazole-3-yl)thio)ethanoic acid and its salts
by: A. S. Hotsulia, et al.
Published: (2020)

Some aspects of synthesis of new 2-((5-furan-2-yl, 2-metylfuran-3-yl)-4-amino-1,2,4-triazole-3-ylthio)acetic acid esters
by: D. M. Danilchenko
Published: (2016)

Synthesis and characterization of benzylidene- [1,3,4]thaidiazol -2-yl-amine
by: Al-Kaddimy H. A. Ahmed
Published: (2006)

Synthesis, physical-chemical properties of 2-((5-(adamantan-1-yl)-4-R-4H-1,2,4-triazole-3-yl)thio)acetic acid esters
by: V. M. Odyntsova
Published: (2017)

Synthesis and physicochemical research of some 2-((5-((theophylline-7'-yl)methyl)-4-R-4H-1,2,4-triazole-3-yl)thio)acetohydrazide ylidenderivatives
by: A. S. Gotsulya, et al.
Published: (2018)

Synthesis and properties of 7-((6-aryl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazol-3-yl)methyl)theophyllines
by: K. D. Bakumovska, et al.
Published: (2023)

The study of UV-spectra of the sodium (3-oxo-3,4-dihydro-2H-[1,2,4]triazino[4,3-c]quinazolin-4-yl)acetate
by: О. V. Kryvoshey
Published: (2016)

Synthesis and properties of S-derivatives of 4-amino-5-(5-methylpyrazol-3-yl)-1,2,4-triazole-3-thiol
by: S. O. Fedotov, et al.
Published: (2021)

Synthesis and transformation in the series of 2-((5-(2,4- and 3,4-dimethoxyphenyl)-3H-1,2,4-triazole-3-yl)thio)acetic acids
by: D. V. Dovbnia, et al.
Published: (2021)

3-(1,2,3-Triazol-4-yl)-β-Carbolines and 3-(1<i>H</i>-Tetrazol-5-yl)-β-Carbolines: Synthesis and Evaluation as Anticancer Agents
by: João L. P. Ribeiro, et al.
Published: (2022)

Anticonvulsant activity 2-((5-(3-(4-fluorophenyl)-4-R2-1,2,4-triazole-3-yl)-thio)-1-arylethanone
by: O. A. Bihdan
Published: (2019)

Antimicrobial screening of new 5-(chromene-3-yl) methylene-2,4-thiazolidinediones
by: Cristina Nastasă, et al.
Published: (2015)

Antimicrobial screening of new 5-(chromene-3-yl)methylene-2,4-thiazolidinediones
by: Cristina Nastas?, et al.
Published: (2015)

Synthesis and antitumor activity of 1,3,4-oxadiazole substituted 2-(5-ylidene-2,4-dioxothiazolidin-3-yl)-acetamides
by: Maryan Lelyukh, et al.
Published: (2023)

Designing, synthesis and bioactivities of 4-[3-(4-hydroxyphenyl)-5-aryl-4,5-dihydro-pyrazol-1-yl]benzenesulfonamides
by: Halise Inci Gul, et al.
Published: (2017)

Synthesis and properties of S-alkyl 4-amino-5-(5-(3-fluorophenyl)-pyrazol-3-yl)-1,2,4-triazole-3-thiol derivatives
by: S. O. Fedotov, et al.
Published: (2023)

The synthesis of N-(4-aryl-thiazol-2-yl)-N1-(4,5,6,7-tetrahydro-3H-azepin-2-yl)-hydrazine hydrobromides and the cardioprotective activity of (41-methoxyphenyl-thiazol-2-yl) derivative
by: Sergii А. Demchenko, et al.
Published: (2021)

Synthesis, physical and chemical properties of esters of 2-((5-(hydroxy(phenyl)methyl)-4-R-1,2,4-triazole-3-yl)thio)ethanoic and 3-(((5-(hydroxy(phenyl)methyl)-4-R-1,2,4-triazole-3-yl)thio)methyl)benzoic acids
by: А. M. Rud, et al.
Published: (2017)

SYNTHESIS AND ANTIOXIDANT ACTIVITY OF (E)-3-(3-(4-OXO-4H-CHROMEN-3-YL)ACRYLOYL) 2H-CHROMEN-2-ONE DERIVATIVES
by: S. S. Shatokhin, et al.
Published: (2021)

Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles
by: I. І. Myrko, et al.
Published: (2021)

Molecular Drug Design, Synthesis and Antibacterial study of Novel 4-Oxothiazolidin-3-yl Derivatives
by: Sarah S. Ismaeel, et al.
Published: (2020)

Synthesis, Characterization and Biological Activity of Some New 4-Substituted-phenyl-3-chloro-1-{5-[(3, 5-dimethyl-1H-pyrazol-1- yl) methyl]-1, 3, 4-thiadiazol-2-yl} azetidin-2-one
by: Rafah Fadhil Al-Smaisim
Published: (2012)

Computer prediction of acute toxicity of thioderivatives of 3,5-bis(5-mercapto-4-R-4H-1,2,4-triazol-3-yl)phenol
by: K. K. Isaicheva, et al.
Published: (2024)

Pharmacological potential of 3,5-dimethyl-4-(3-(5-nitrofuran-2-yl)allylidenamino)-1-alkyl-1,2,4-triazolium bromides
by: A. S. Hotsulia, et al.
Published: (2024)

Development of determination method and study of piperidinium 2-((5-(furan-2-yl)-4-phenyl-4H-1,2,4-triazol-3-yl)thio) acetate in milk of cows in 12 hours after administration
by: B. O. Varynskyi, et al.
Published: (2019)

The study of antimicrobial and antifungal activity of Nʹ-ylidene-2(3-(adamantan-1-yl)-1H-1,2,4-triazole-5-yl)thioacetohydrazides
by: V. M. Odyntsova
Published: (2015)