Results 51 to 60 of about 10,618 (207)

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

British Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown, Alan Armstrong, David J. Mann   +2 more
wiley   +1 more source

Synthesis and Anti-inflammatory Activity of Some Novel 3-(6-Substituted-1, 3-benzothiazole-2-yl)-2-[{(4-substituted phenyl) amino} methyl] quinazolines-4 (3H)-ones

E-Journal of Chemistry, 2009
A series of novel 3-(6-substituted-1, 3-benzothiazole-2-yl)-2-[{(4-substituted phenyl) amino} methyl] quinazolines-4(3H)-ones were synthesized by treating 2-(chloromethyl)-3-(6-substituted-1, 3-benzothiazole-2-yl) quinazoline-4-(3H)-one (IIa-d) with ...
Manish Srivastav, MD. Salahuddin, S. M. Shantakumar   +2 more
doaj   +1 more source

ADAM17 and its proteolytic targets in disease pathogenesis

The FEBS Journal, EarlyView.
ADAM17 as a multifunctional sheddase with contrasting roles across inflammatory, metabolic, cardiovascular, and neoplastic diseases. Through regulated activation by iRhom, iTAP/FRMD8, and tetraspanins, ADAM17 cleaves diverse membrane ligands and receptors, thereby promoting inflammation, fibrosis, obesity, insulin resistance, and tumor progression ...
Abdulbasit Amin, Marina Badenes
wiley   +1 more source

Molecular Docking and Anticonvulsant Activity of Newly Synthesized Quinazoline Derivatives

Molecules, 2017
A new series of quinazoline-4(3H)-ones are evaluated for anticonvulsant activity. After intraperitoneal (ip) injection to albino mice at a dose of 100 mg/kg body weight, synthesized quinazolin-4(3H)-ones (1–24) were examined in the maximal electroshock ...
Hatem A. Abuelizz, Rabab El Dib, Mohamed Marzouk, El-Hassane Anouar, Yousreya A. Maklad, Hanan N. Attia, Rashad Al-Salahi   +6 more
doaj   +1 more source

Design, Synthesis, and In vitro Antitumor Activity Evaluation of Novel 4‐pyrrylamino Quinazoline Derivatives [PDF]

, 2011
Peer Reviewedhttp://deepblue.lib.umich.edu/bitstream/2027.42/88050/1/j.1747-0285.2011.01234.x ...
Ji, Min, Li, Mingdong, Lian, Jiqin, Tang, Wenhua, Wu, Xiaoqing, Xu, Liang, Zheng, Youguang   +6 more
core   +1 more source

Efficacy and safety of fruquintinib combined with albumin‐bound paclitaxel as second‐line therapy for advanced gastric cancer following failure of PD‐1 inhibitor‐containing treatment (TACTIC GC‐01): A phase II single‐arm study

International Journal of Cancer, Volume 158, Issue 9, Page 2219-2228, 1 May 2026.
What's new? Anti‐angiogenic drugs have shown promising efficacy as a second‐line treatment for advanced gastric cancer. However, it remains unclear how alterations in the tumor microenvironment following first‐line immunotherapy may impact tumor angiogenesis and influence subsequent therapeutic outcomes. This single‐arm study prospectively explored the
Xiaoting Ma, Kai Ou, Xiu Liu, Biyang Cao, Wenwei Yang, Jingyu Lu, Letian Zhang, Qi Wang, Lizhen Gao, Zhichao Jiang, Yongkun Sun, Lin Yang   +11 more
wiley   +1 more source

Behavioural Response of Triatoma infestans (Klug) (Hemiptera: Reduviidae) to Quinazolines

Molecules, 2005
The behavioural responses of the haematophagous bug Triatoma infestans towards some previously identified components of its faeces: 4-methylquinazoline, 2,4- dimethylquinazoline and their mixtures were evaluated using a video tracking system.
E. Zerba, A. Cork, D. Fernández, P. Santo Orihuela, H. Masuh, F. Camps, A. Fontán, R. A. Alzogaray   +7 more
doaj   +1 more source

Synthesis and anticancer activities of diquinazoline diselenides compounds [PDF]

, 2016
A series of novel diquinazoline diselenide compounds was designed and synthesized with substituted 4-chloroquinazoline and sodium diselenide. Their structures were confirmed by IR, 1H NMR, 13C NMR, and elemental analyses.The antitumor activity of the new
Cao, Kun, Huang, YinJiu, Ji, ChunNuan, Liu, Gang, Liu, XiGuang, Sun, Lin, Xu, ShengGuang   +6 more
core  

A Review of Quinazoline-Based EGFR/VEGFR-2 Dual Inhibitors as Potent Anticancer Agents: Structure-Activity Relationship and Docking Studies [PDF]

Pharmaceutical Sciences
The epidermal growth factor receptor (EGFR) is a receptor tyrosine kinase (RTK) that initiates various signaling pathways resulting in processes such as gene expression, proliferation, angiogenesis, and inhibition of apoptosis.
Fatemeh Yousefbeyk, Saeed Ghasemi
doaj   +1 more source

Systematic Kinase Inhibitor Profiling Identifies CDK9 as a Synthetic Lethal Target in NUT Midline Carcinoma [PDF]

, 2017
Kinase inhibitors represent the backbone of targeted cancer therapy, yet only a limited number of oncogenic drivers are directly druggable. By interrogating the activity of 1,505 kinase inhibitors, we found that BRD4-NUT-rearranged NUT midline carcinoma (
Albert, Alekseyenko, Barretina, Baumli, Buettner, Bösken, Chan, Chen, Elkins, Fece de la Cruz, Filippakopoulos, Flaherty, French, Garnett, Grayson, Gregory, Greifenberg, Hortobagyi, Hu, Huang, Hyman, Iorio, Itzen, Kandoth, Kumar, Lam, Lemke, Lorenzin, Lu, Martins, McLornan, Morales, Nojima, Odawara, Reynoird, Riniker, Rosell, Rossi, Seashore-Ludlow, Shaw, Sos, Sos, Squires, Stathis, Stock, Van Cutsem, Walsby, Yan, Yu, Zhang, Zhang, Zou   +51 more
core   +2 more sources