Vanillin-based indolin-2-one derivative bearing a pyridyl moiety as a promising anti-breast cancer agent via anti-estrogenic activity

O Bender, I Celik, R Dogan, A Atalay, ME Shoman… - ACS …, 2023 - ACS Publications
The structure-based design introduced indoles as an essential motif in designing new
selective estrogen receptor modulators employed for treating breast cancer. Therefore, here …

Discovery of oxindole‐based FLT3 inhibitors as a promising therapeutic lead for acute myeloid leukemia carrying the oncogenic ITD mutation

O Bender, ME Shoman, TFS Ali, R Dogan… - Archiv der …, 2023 - Wiley Online Library
FMS‐like tyrosine kinase 3 (FLT3) mutations occur in approximately 30% of acute myeloid
leukemia (AML) patients. In the current study, the oxindole chemotype is employed as a …

Virtual screening identifies irreversible FMS-like tyrosine kinase 3 inhibitors with activity toward resistance-conferring mutations

D Bensinger, D Stubba, A Cremer, V Kohl… - Journal of Medicinal …, 2019 - ACS Publications
The use of covalent irreversible binding inhibitors is an established concept for drug
development. Usually, the discovery of new irreversible kinase inhibitors occurs …

The Employment of Sodium Hydride as a Michael Donor in Palladium‐catalyzed Reductions of α, β‐Unsaturated Carbonyl Compounds

Y Liu, Y Mao, Y Hu, J Gui, L Wang… - Advanced Synthesis …, 2019 - Wiley Online Library
Sodium hydride was employed as a Michael donor under the catalysis of PdCl2 for 1, 4‐
conjugate reductions of α, β‐unsaturated carbonyl compounds, which features operational …

Free fatty acid receptor 1 (GPR40) agonists containing spirocyclic periphery inspired by LY2881835

M Krasavin, A Lukin, D Bagnyukova, N Zhurilo… - Bioorganic & Medicinal …, 2016 - Elsevier
The free fatty acid receptor 1 (FFA1), a G protein-coupled receptor (GPCR) naturally
activated by long-chain fatty acids is a novel target for the treatment of metabolic diseases …

Indolinone based LRRK2 kinase inhibitors with a key hydrogen bond

S Göring, JM Taymans, V Baekelandt… - Bioorganic & Medicinal …, 2014 - Elsevier
The most prevalent leucine-rich repeat kinase 2 (LRRK2) mutation G2019S is associated
with Parkinson's disease (PD). It enhances kinase activity and has been identified in both …

Discovery and Anticancer Screening of Novel Oxindole-Based Derivative Bearing Pyridyl Group as Potent and Selective Dual FLT3/CDK2 Kinase Inhibitor

A Soudi, O Bender, I Celik, AAA El-Hafeez, R Dogan… - Pharmaceuticals, 2024 - mdpi.com
Protein kinases regulate cellular activities and make up over 60% of oncoproteins and proto-
oncoproteins. Among these kinases, FLT3 is a member of class III receptor tyrosine kinase …

Evaluation of virtual screening strategies for the identification of γ-secretase inhibitors and modulators

A Ioppolo, M Eccles, D Groth, G Verdile, M Agostino - Molecules, 2021 - mdpi.com
γ-Secretase is an intramembrane aspartyl protease that is important in regulating normal cell
physiology via cleavage of over 100 transmembrane proteins, including Amyloid Precursor …

An efficient multigram-scale synthesis of 4-(ω-chloroalkoxy) phenols

AI Zinin, EV Stepanova, U Jost, NN Kondakov… - Russian Chemical …, 2017 - Springer
Efficient multigram two-step syntheses of 4-(2-chloroethoxy) phenol and 4-(3-chloropropoxy)
phenol in> 70% yields starting from 4-hydroxybenzaldehyde and reagents with general …

Synthesis and In Vitro Photodynamic Activity of Cationic Boron Dipyrromethene-Based Photosensitizers Against Methicillin-Resistant Staphylococcus aureus

P Dharmaratne, RCH Wong, J Wang, PC Lo, B Wang… - Biomedicines, 2020 - mdpi.com
A series of cationic boron dipyrromethene (BODIPY) derivatives were synthesized and
characterized with various spectroscopic methods. Having the ability to generate singlet …