Results 61 to 70 of about 7,050 (179)

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

Quinazolinone and quinazoline derivatives: recent structures with potent antimicrobial and cytotoxic activities

Research in Pharmaceutical Sciences, 2016
The heterocyclic compounds have a great importance in medicinal chemistry. One of the most important heterocycles in medicinal chemistry are quinazolines possessing wide spectrum of biological properties like antibacterial, antifungal, anticonvulsant ...
Elham Jafari, Marzieh Rahmani Khajouei, Farshid Hassanzadeh, Gholam Hossein Hakimelahi, Ghadam Ali Khodarahmi   +4 more
doaj  

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

Antiproliferative and Antiangiogenic Properties of New VEGFR-2-targeting 2-thioxobenzo[g]quinazoline Derivatives (In Vitro)

Molecules, 2020
A series of 3-ethyl(methyl)-2-thioxo-2,3-dihydrobenzo[g]quinazolines (1–17) were synthesized, characterized, and evaluated in vitro for their antiangiogenesis VEGFR-2-targeting, antiproliferative, and antiapoptotic activities against breast MCF-7 and ...
Hatem A. Abuelizz, Mohamed Marzouk, Ahmed H. Bakheit, Hanem M. Awad, Maha M. Soltan, Ahmed M. Naglah, Rashad Al-Salahi   +6 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

Design, Synthesis, and Cytotoxicity Evaluation of Novel Indolin-2-One Based Molecules on Hepatocellular Carcinoma HepG2 Cells as Protein Kinase Inhibitors

Molecules
A series of indolinone-based derivatives were designed and synthesized using the hybrid pharmacophoric design approach as cytotoxic kinase inhibitors.
Manal M. Kandeel, Mohamed Kamal AbdElhameid, Mohamed Adel, Muhammad Y. Al-Shorbagy, Ahmed T. Negmeldin   +4 more
doaj   +1 more source

Design, Synthesis, and Biological Evaluation of 4-aminoquinazoline Appended-Benzofuran Hybrids as Epidermal Growth Factor Receptor Inhibitors

Proceedings, 2019
Nitrogen-containing heterocycles such as quinazolines and benzofurans have received a great amount of interest in targeted therapies as antitumor drugs [1]. [...]
Marole Maria Maluleka, Malose Jack Mphahlele   +1 more
doaj   +1 more source

Fruquintinib Plus TAS‐102 With or Without SBRT as Third‐ Or Later‐Line Therapy for Metastatic Colorectal Cancer: Preliminary Results From a Prospective Phase II Trial

Cancer Medicine, Volume 15, Issue 5, May 2026.
ABSTRACT Both fruquintinib and TAS‐102 monotherapies are guideline‐recommended for third‐line treatment of metastatic colorectal cancer (mCRC). This study aimed to analyze the preliminary outcomes of fruquintinib combined with TAS‐102, with or without stereotactic body radiation therapy (SBRT), as a third‐ or later‐line therapy for mCRC.
Yi Wang, Jianfen Xu, Linchun Liang, Yunjie Chen, Leizheng Fei, Jing Hu, Jianjiong Li, Yi Lu, Feng Ren, Ke Chen, Yanping Shen, Qingsong Tao, Zhi Fang, Kaitai Liu, Hua Ye, Jing Zhang, Yunbao Xu, Haoxun Mao, Chen Zhang, Chuangzhou Rao   +19 more
wiley   +1 more source

Quinazoline compounds for antitumor treatment

Experimental Oncology, 2023
Summary. Quinazolines are among the most useful heterocyclic compounds due to their diverse chemical reactivity and a wide range of biological activity. Despite a large number of publications devoted to quinazolines and their derivatives, information is presented predominantly regarding the features of the synthesis of these compounds and their ...
openaire   +2 more sources

Recent advances in 4-aminoquinazoline based scaffold derivatives targeting EGFR kinases as anticancer agents

Future Journal of Pharmaceutical Sciences, 2016
Quinazoline derivatives are fused heterocyclic ring systems which have been explored for their inhibitory activity towards various protein kinase enzymes and their role as anticancer agents.
Rania S.M. Ismail, Nasser S.M. Ismail, Sahar Abuserii, Dalal A. Abou El Ella   +3 more
doaj   +1 more source