Results 51 to 60 of about 18,476 (212)

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

Absolute Configurations and Chitinase Inhibitions of Quinazoline-Containing Diketopiperazines from the Marine-Derived Fungus Penicillium polonicum

Marine Drugs, 2020
Three new quinazoline-containing diketopiperazines, polonimides A–C (1–3), along with four analogues (4–7), were obtained from the marine-derived fungus Penicillium polonicum.
Xing-Chen Guo, Ya-Hui Zhang, Wen-Bin Gao, Li Pan, Hua-Jie Zhu, Fei Cao   +5 more
doaj   +1 more source

Targeting kinases with anilinopyrimidines: Discovery of N-phenyl-N'-[4-(pyrimidin-4-ylamino)phenyl]urea derivatives as selective inhibitors of class III receptor tyrosine kinase subfamily [PDF]

, 2015
Kinase inhibitors are attractive drugs/drug candidates for the treatment of cancer. The most recent literature has highlighted the importance of multi target kinase inhibitors, although a correct balance between specificity and non-specificity is ...
Chilin, Adriana, DALLA VIA, Martina, Ferrarese, Alessandro, Gandin, Valentina, Marzano, Cristina, Marzaro, Giovanni   +5 more
core   +2 more sources

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

Afatinib use in recurrent epithelial ovarian carcinoma. [PDF]

, 2019
•Genomic tumor testing is an important tool in guiding treatment for gynecologic malignancies.•Targetable mutations may lead to new therapies in gynecologic cancer treatment.•Her2/neu mutations in serous ovarian carcinomas can be targeted with ERBB2 ...
Alvarez, Edwin A, Hanft, Wyatt J, Kennedy, Vanessa A, Shepherd-Littlejohn, Amanda L   +3 more
core   +1 more source

Asymmetric Negishi and Kumada Couplings

Advanced Synthesis &Catalysis, Volume 368, Issue 5, 3 March 2026.
This review summarizes asymmetric Negishi and Kumada cross‐coupling reactions from the 1980s through 2025. It examines enantioselective and enantiospecific transformations catalyzed by nickel, palladium, and cobalt complexes , highlighting ligand design, mechanistic insights, and applications in constructing complex chiral molecules and natural ...
Rui‐Heng Wang, Aishun Ding, Ramon Rios
wiley   +1 more source

Integrated CO2 capture-fixation chemistry via interfacial ionic liquid catalyst in laminar gas/liquid flow [PDF]

, 2019
Simultaneous capture of carbon dioxide (CO2) and its utilization with subsequent work-up would significantly enhance the competitiveness of CO2-based sustainable chemistry over petroleum-based chemistry.
Babu, A.G., Hwang, Y.-H., Kim, D.-P., Kim, J.-O., Ko, D.-H., Singh, A.K., Vishwakarma, N.K.   +6 more
core   +1 more source

Direct‐to‐Biology: Streamlining the Path From Chemistry to Biology in Drug Discovery

ChemMedChem, Volume 21, Issue 4, 25 February 2026.
Crude yet clever: Direct‐to‐biology workflows exploit nanoscale synthesis and plate‐based assays to accelerate hit discovery, save precious intermediates, and rethink early drug discovery. Direct‐to‐biology (D2B) has emerged as a transformative concept in early drug discovery, defined by the direct on‐target screening of crude reaction mixtures without
Ariane F. Hübner, Fabian Barthels
wiley   +1 more source

Recent Advances in Structural Optimization of Quinazoline-Based Protein Kinase Inhibitors for Cancer Therapy (2021–Present)

Molecules
Cancer is a complicated, multifaceted disease that can impact any organ in the body. Various chemotherapeutic agents have a low selectivity and are very toxic when used alone or in combination with others.
Heba T. Abdel-Mohsen, Manal M. Anwar, Nesreen S. Ahmed, Somaia S. Abd El-Karim, Sameh H. Abdelwahed   +4 more
doaj   +1 more source

Polymethoxylated N‐Carboranyl Isoquinolinones: A New Scaffold for ABCG2 Inhibitors

ChemMedChem, Volume 21, Issue 3, 12 February 2026.
Combinations of a boron‐based clusters (carborane) and polymethoxy group patterns are crucial to overcome ABCG2‐mediated multidrug resistance in cancer cells. (Created in BioRender. Kuhnert, L. (2025) https://BioRender.com/h4cnh5m). ABCG2‐mediated multidrug resistance (MDR) is a major challenge among chemotherapeutic treatments of colon, pancreatic ...
Lydia Kuhnert, Philipp Stockmann, Peter Lönnecke, Mara Anna Wolniewicz, Evamarie Hey‐Hawkins, Walther Honscha   +5 more
wiley   +1 more source