Synthesis and biological assessment of indole derivatives containing penta-heterocycles scaffold as novel anticancer agents towards A549 and K562 cells

G Zhang, Z Tang, S Fan, C Li, Y Li, W Liu… - Journal of Enzyme …, 2023 - Taylor & Francis
Herein, a new series of 2-chloro-N-(5-(2-oxoindolin-3-yl)-4 H-pyrazol-3-yl) acetamide
derivatives containing 1, 3, 4-thiadiazole (10a–i) and 4 H-1, 2, 4-triazol-4-amine (11a–r) …

Design, synthesis and Molecular modeling study of certain EGFR inhibitors with a quinazolinone scaffold as anti-hepatocellular carcinoma and Radio-sensitizers

WM Ghorab, SA El-Sebaey, MM Ghorab - Bioorganic Chemistry, 2023 - Elsevier
A set of novel N-substituted-2-((4-oxo-3-phenyl-3, 4-dihydroquinazolin-2-yl) thio) acetamide
3–16 were designed and synthesized from 2-mercapto-3-phenylquinazolinone 2. The …

Development of penipanoid C-inspired 2-benzoyl-1-methyl-2, 3-dihydroquinazolin-4 (1H)-one derivatives as potential EGFR inhibitors: Synthesis, anticancer …

K Veena, MS Raghu, KY Kumar, KA Dahlous… - Journal of Molecular …, 2022 - Elsevier
A novel class of penipanoid C-inspired 2-benzoyl-1-methyl-2, 3-dihydroquinazolin-4 (1H)-
ones (3a-3f) and 1-methyl-2-(3, 4, 5-trihydroxybenzoyl)-2, 3-dihydroquinazolin-4 (1H)-one …

[HTML][HTML] Enzymatic synthesis of fluorinated compounds

X Cheng, L Ma - Applied Microbiology and Biotechnology, 2021 - Springer
Fluorinated compounds are widely used in the fields of molecular imaging, pharmaceuticals,
and materials. Fluorinated natural products in nature are rare, and the introduction of …

Synthesis and preliminary structure-activity relationship study of 3-methylquinazolinone derivatives as EGFR inhibitors with enhanced antiproliferative activities …

Y Zhang, Q Wang, L Li, Y Le, L Liu, J Yang… - Journal of Enzyme …, 2021 - Taylor & Francis
In this paper, a set of 3-methylquniazolinone derivatives were designed, synthesised, and
studied the preliminary structure-activity relationship for antiproliferative activities. All target …

EGFR/VEGFR-2 dual inhibitor and apoptotic inducer: Design, synthesis, anticancer activity and docking study of new 2-thioxoimidazolidin-4one derivatives

AAE Mourad, NA Farouk, ESH El-Sayed, ARE Mahdy - Life Sciences, 2021 - Elsevier
Aims EGFR and VEGFR-2 have emerged as promising targets for cancer management as
they play a crucial role in tumor growth, angiogenesis and metastasis. A novel series of 2 …

Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer …

MW Aziz, AM Kamal, KO Mohamed… - Bioorganic & medicinal …, 2021 - Elsevier
New acetamide (IV ae) and 1, 3-thiazolidinone derivatives (VII ae) were designed,
synthesized and assessed for their cytotoxic activity against MCF-7 and A549 cell lines …

Development of Imidazo [1, 2-a] pyridine-based probe for detection of hydrazine and its applications in imaging of HepG2 cell

D Li, Q Wang, N Rao, Y Zhang, Y Le, L Liu, L Li… - Journal of Molecular …, 2021 - Elsevier
A novel fluorescent probe IMPD based on imidazo [1, 2-a] pyridine for detection of hydrazine
was designed and synthesized. This probe used maleimide as the recognition group, which …

Design, synthesis and biological evaluation of 4-arylamino-pyrimidine derivatives as focal adhesion kinase inhibitors

Z Long, Y Zuo, R Li, Y Le, Y Dong, L Yan - Bioorganic Chemistry, 2023 - Elsevier
A novel series of 4-arylamino-pyrimidine derivatives were designed and synthesized as
focal adhesion kinase (FAK) inhibitors under the strategy of structure-based drug design …

Design, synthesis and antitumor activity of 5-trifluoromethylpyrimidine derivatives as EGFR inhibitors

Y Zuo, R Li, Y Zhang, G Bao, Y Le… - Journal of Enzyme …, 2022 - Taylor & Francis
A new series of 5-trifluoromethylpyrimidine derivatives were designed and synthesised as
EGFR inhibitors. Three tumour cells A549, MCF-7, PC-3 and EGFR kinase were employed …