Results 51 to 60 of about 387 (133)

Single‐Sequence Deep Learning Delivers Crystal‐Quality Models of Covalent K‐Ras G12 Hotspot Complexes

IUBMB Life, Volume 78, Issue 6, June 2026.
ABSTRACT Structure‐based design of covalent drugs has achieved tremendous success by understanding and leveraging the three‐dimensional interactions between small‐molecule drug candidates and their protein targets. However, this approach traditionally relies on high‐resolution co‐complex structures obtained by X‐ray crystallography, NMR, or cryo‐EM ...
Sungwon Jung, Qinheng Zheng, Kevan M. Shokat   +2 more
wiley   +1 more source

Biological evaluation of novel 6-Arylbenzimidazo [1,2-c] quinazoline derivatives as inhibitors of LPS-induced TNF- alpha secretion

Biological Research, 2008
This study describes the effect of novel 6-Arylbenzimidazo [1,2-c] quinazoline derivatives as tumor necrosis factor alpha (TNF-á) production inhibitors.
GLORIA D GALARCE, ROCÍO E FONCEA, ANA M EDWARDS, HERNÁN PESSOA-MAHANA, CARLOS D PESSOA-MAHANA, ROBERTO A EBENSPERGER   +5 more
doaj  

Exploring Quinazoline as a Scaffold for Developing Novel Therapeutics in Alzheimer’s Disease

Molecules
Quinazoline, a privileged scaffold in medicinal chemistry, offers promising potential in the synthesis of anti-Alzheimer’s disease (AD) drugs. This heterocyclic compound, characterized by its fused benzene and pyrimidine rings, enables the design of ...
Qais Abualassal, Zead Abudayeh, Ala’ Sirhan, Abdulrahman Mkia   +3 more
doaj   +1 more source

A Feasibility Study of the Repurposing of Prazosin to Improve Treatment Outcomes in Men Receiving Radiotherapy for Prostate Cancer (MiniRaP‐00)

The Prostate, Volume 86, Issue 8, Page 891-899, June 2026.
ABSTRACT Background Further work is needed to improve treatment outcomes for prostate cancer (PCa), with the repurposing of the α1‐adrenoreceptor antagonists presenting a potential solution. This feasibility clinical trial presents the first prospective data of the use of an α1‐adrenoreceptor antagonist in men undergoing radiotherapy for PCa.
Liam D. King, David Christie, Daniel Cehic, Wendy Dare, Russ Chess‐Williams, Donna Sellers, Catherine McDermott, Alexandra McCarthy, Shailendra Anoopkumar‐Dukie   +8 more
wiley   +1 more source

Synthesis And Antimicrobial Activity Of Some Annelated Quinazoline Derivatives [PDF]

Zeitschrift für Naturforschung B, 2006
A highly efficient and versatile synthetic approach to the synthesis of annelated quinazoline derivatives viz. 3,4,9,10a-tetraazaphenanthrenes 5 - 7, thiazolidinylquinazoline 9, 2,4,9,10a-tetraazaphenanthrene 11, quinazolino[4,3-b]quinazolin-8-one 12 and imidazoquinazolines 14a,b, 15.
openaire   +1 more source

Design, Synthesis of Novel Quinazolinone Derivatives and Evaluation of EGFR Kinase Inhibition Activity via In Vitro and In Silico Studies

Chemical Biology &Drug Design, Volume 107, Issue 6, June 2026.
Seventeen new quinazolinone derivatives were synthesized in pure form. Compound 4j showed the highest inhibitory activity against the A549 cell line and induced apoptosis via caspase‐3 activation in MCF‐7 cells. 4j inhibited EGFR enzyme twice as effectively as gefitinib.
Aybüke Züleyha Kaya, Asaf Evrim Evren, Gülşen Akalın‐Çiftçi, Leyla Yurttaş   +3 more
wiley   +1 more source

Access to Original Vinylic Chlorides in the Quinazoline Series via a Monoelectronic Transfer Reaction Approach

Molecules, 2010
A series of new quinazoline derivatives bearing a vinylic chloride group on the 2-position was prepared by using a consecutive SRN1 / ERC1 radical strategy.
Martine Maillard-Boyer, Caroline Castera-Ducros, Pierre Verhaeghe, France Sifredi, Pascal Rathelot, Patrice Vanelle   +5 more
doaj   +1 more source

Cruzain Inhibitors for Chagas Disease: Anticorrelated Optimisation Landscapes and the Multiparametric Path to Clinical Candidates

Chemical Biology &Drug Design, Volume 107, Issue 6, June 2026.
Three decades of cruzain‐targeted drug discovery have yielded 215 sub‐micromolar inhibitors but no clinical candidates. This review diagnoses a systemic translational failure driven by single‐parameter optimisation and proposes a multiparametric framework integrating enzymatic potency, cathepsin selectivity, intracellular exposure, and metabolic ...
Caroline Rodrigues Chaves dos Reis, Hellen Valério Chaves Moura de Souza, Lidia Corrêa Parra, Guilber Valério Chaves Moura de Souza, Bruna Costa Zorzanelli, Nubia Boechat, Lucas Villas Bôas Hoelz, Tácio Vinício Amorim Fernandes   +7 more
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

Thermo‐Fluorescent Bactericidal Quantum Dots Based Smart Multifunctional Textiles via Molecular Surface Engineering and 3D‐Printed Interlocked Architectures

Advanced Healthcare Materials, Volume 15, Issue 19, 22 May 2026.
A versatile approach is presented for fabricating smart multifunctional textiles by integrating thermo‐fluorescent carbon dot/polymer nanocomposite coatings with 3D‐printed interlocked architectures. The fabrics exhibit temperature‐responsive fluorescence, durable hydrophobicity, strong antibacterial and antioxidant activity, and enhanced UV protection.
Poushali Das, Sayan Ganguly, Parham Khoshbakht Marvi, Misha Muthalali, Fatemeh Parniani, Shiza Hassan, Xiaowu (Shirley) Tang, Seshasai Srinivasan, Amin Reza Rajabzadeh   +8 more
wiley   +1 more source