Review on EGFR inhibitors: critical updates

D Singh, BK Attri, RK Gill… - Mini reviews in medicinal …, 2016 - ingentaconnect.com
Epidermal Growth Factor Receptor (EGFR) is a transmembrane glycoprotein that constitutes
one of the four members of ErbB family of tyrosine kinase receptors. Activation of EGFR …

Challenges and perspectives on the development of small-molecule EGFR inhibitors against T790M-mediated resistance in non-small-cell lung cancer …

Z Song, Y Ge, C Wang, S Huang, X Shu… - Journal of medicinal …, 2016 - ACS Publications
Because of the development of drug-resistance mutations, particularly the “gatekeeper”
threonine790-to-methionine790 (T790M) mutation in the ATP-binding pocket of the …

Structure-based design and synthesis of covalent-reversible inhibitors to overcome drug resistance in EGFR

D Basu, A Richters, D Rauh - Bioorganic & Medicinal Chemistry, 2015 - Elsevier
The clinical success of covalent kinase inhibitors in the treatment of EGFR-dependent non-
small cell lung cancer (NSCLC) has rejuvenated the appreciation of reactive small …

Design, synthesis and biological evaluation of nitric oxide-releasing 5-cyano-6-phenyl-2, 4-disubstituted pyrimidine derivatives

L Chi, H Wang, F Yu, C Gao, H Dai, X Si, Y Dong… - Bioorganic & Medicinal …, 2023 - Elsevier
In this study, a series of nitric oxide (NO)-releasing 5-cyano-6-phenyl-2, 4-disubstituted
pyrimidine derivatives were designed and synthesized. In the in vitro biological evaluation …

Generation of BT-Amide, a Bone-Targeted Pyk2 Inhibitor, Effective via Oral Administration, for the Prevention of Glucocorticoid-Induced Bone Loss

X Wang, AY Sato, S Marino, N Akel… - Journal of Medicinal …, 2024 - ACS Publications
Glucocorticoid-induced osteoporosis (GIOP) is the leading cause of iatrogenic osteoporosis
due to the widespread clinical use of glucocorticoids (GC) as immunosuppressants …

Protein kinase inhibitor-based cancer therapies: Considering the potential of nitric oxide (NO) to improve cancer treatment

S Ghione, N Mabrouk, C Paul, A Bettaieb… - Biochemical …, 2020 - Elsevier
The deregulation of a wide variety of protein kinases is associated with cancer cell initiation
and tumor progression. Owing to their indispensable function in signaling pathways driving …

Design and synthesis of new hybrids from 2-cyano-3, 12-dioxooleana-9-dien-28-oic acid and O2-(2, 4-dinitrophenyl) diazeniumdiolate for intervention of drug …

F Kang, Y Ai, Y Zhang, Z Huang - European Journal of Medicinal Chemistry, 2018 - Elsevier
To search for new drugs for intervention of drug-resistant lung cancer, a series of hybrids 4-
15 from 2-cyano-3, 12-dioxooleana-9-dien-28-oic acid (CDDO) and O 2-(2, 4-dinitrophenyl) …

Oleanolic acid-NO donor-platinum (II) trihybrid molecules: Targeting cytotoxicity on hepatoma cells with combined action mode and good safety

L Fang, M Feng, F Chen, X Liu, H Shen, J Zhao… - Bioorganic & Medicinal …, 2016 - Elsevier
By taking advantage of good affinity of oleanolic acid (OA) to the bile acid transporter, a
series of hybrid compounds from oleanolic acid (OA) or OA-nitric oxide (NO) donor …

Recent development of the second and third generation irreversible epidermal growth factor receptor inhibitors

W Han, Y Du - Chemistry & Biodiversity, 2017 - Wiley Online Library
Recent reports suggested that essential directions for new lung cancer, breast carcinoma
therapies, as well as the roomier realm of targeted cancer therapies were provided through …

An overview of phenylsulfonylfuroxan-based nitric oxide donors for cancer treatment

C Gao, X Li, T Liu, W Wang, J Wu - Bioorganic Chemistry, 2024 - Elsevier
Nitric oxide (NO) is a gaseous molecule integral to numerous physiological processes,
including tumor modulation, cardiovascular regulation, and systemic physiological functions …