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Design and synthesis of selective FLT3 inhibitors via exploration of back pocket II

Publikováno v: Future Medicinal Chemistry. 15:57-71

Aim: The clinical benefits of FLT3 inhibitors against acute myeloid leukemia (AML) have been limited by selectivity and resistance mutations. Thus, to identify FLT3 inhibitors possessing high selectivity and potency is of necessity. Methods & results

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e4e2c6feedaad9225b8c2e4b4b234b20
https://doi.org/10.4155/fmc-2022-0231

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Scaffold-hopping of Linifanib to Design 6-Phenylisoxazolo[3,4-b]pyridin-3-amine Derivatives as FLT3 Inhibitors for Treating Acute Myeloid Leukemia

Publikováno v: Letters in Drug Design & Discovery. 20

Background: Acute myeloid leukemia (AML) is the most common type of blood cancer. Fms-like tyrosine kinase 3 (FLT3) is a member of the class III receptor tyrosine kinase family. Overexpression of FLT3 was found in 70-100% of patients with acute myelo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9250921b9447897024d7ae8b81f00588
https://doi.org/10.2174/1570180820666230519140242

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Medicinal Chemistry Strategies for the Development of Bruton’s Tyrosine Kinase Inhibitors against Resistance

Autor: Shan-Liang Sun, Shi-Han Wu, Ji-Bo Kang, Yi-Yuan Ma, Lu Chen, Peng Cao, Liang Chang, Ning Ding, Xin Xue, Nian-Guang Li, Zhi-Hao Shi

Publikováno v: Journal of Medicinal Chemistry. 65:7415-7437

Despite significant efficacy, one of the major limitations of small-molecule Bruton's tyrosine kinase (BTK) agents is the presence of clinically acquired resistance, which remains a major clinical challenge. This Perspective focuses on medicinal chem

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::36ca716b6e50609f90af565ee8a6209b
https://doi.org/10.1021/acs.jmedchem.2c00030

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Synthesis and Biological Evaluation of 2-Amino-1-phenyl-benzimidazole Derivatives as BACE1 Inhibitors

Publikováno v: Letters in Drug Design & Discovery. 20

Background: Alzheimer’s disease (AD), a chronic neurodegenerative disorder predominantly occurs among the elderly, is the leading cause of dementia. The accumulation of β-amyloid (Aβ) is considered the main pathogenies of AD, and β-site APP-clea

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::39196b9a437c00d50c0a0593f56125f8
https://doi.org/10.2174/1570180820666230223151850

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Synthesis and biological evaluation of 4-(4-aminophenyl)-6-methylisoxazolo[3,4-b] pyridin-3-amine covalent inhibitors as potential agents for the treatment of acute myeloid leukemia

Publikováno v: Bioorganicmedicinal chemistry. 70

Fms-like tyrosine kinase 3 (FLT3) mutation has been strongly associated with increased risk of relapse, and the irreversible covalent FLT3 inhibitors had the potential to overcome the drug-resistance. In this study, a series of simplified 4-(4-aminop

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f183b4608b5e09496d050351a434d1ef
https://pubmed.ncbi.nlm.nih.gov/35863236

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Gaining Selectivity in the Back Pocket of Fms-Like Tyrosine Kinase 3: A Case Study

Publikováno v: SSRN Electronic Journal.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4ba92a64463608f95f2e79a31fbaebdf
https://doi.org/10.2139/ssrn.4079721

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