Current scenario of pyrazole hybrids with in vivo therapeutic potential against cancers

Z Xu, Y Zhuang, Q Chen - European Journal of Medicinal Chemistry, 2023 - Elsevier
Chemotherapeutics occupy a pivotal role in the medication of different types of cancers, but
the prevalence and mortality rates of cancer remain high. The drug resistance and low …

A review: FDA-approved fluorine-containing small molecules from 2015 to 2022

N Sheikhi, M Bahraminejad, M Saeedi… - European Journal of …, 2023 - Elsevier
Fluorine-containing small molecules have occupied an especial position in drug discovery
research. The successful clinical use of fluorinated corticosteroids in the 1950s and …

Discovery of Pyrazolo[3,4-d]pyridazinone Derivatives as Selective DDR1 Inhibitors via Deep Learning Based Design, Synthesis, and Biological Evaluation

X Tan, C Li, R Yang, S Zhao, F Li, X Li… - Journal of medicinal …, 2021 - ACS Publications
Alterations of discoidin domain receptor1 (DDR1) may lead to increased production of
inflammatory cytokines, making DDR1 an attractive target for inflammatory bowel disease …

[HTML][HTML] In search of novel inhibitors of anti-cancer drug target fibroblast growth factor receptors: Insights from virtual screening, molecular docking, and molecular …

A Mahfuz, MA Khan, S Biswas, S Afrose… - Arabian Journal of …, 2022 - Elsevier
Fibroblast growth factor receptors (FGFR) are an essential player in oncogenesis and tumor
progression. LY2874455 was identified as a pan-FGFR inhibitor and has gone through …

Design, synthesis, and antiviral activities of myricetin derivatives containing pyridazinone

L Xing, Y An, Y Qin, H Xin, T Deng, K Meng… - New Journal of …, 2024 - pubs.rsc.org
26 derivatives of myricetin containing pyridazinone were designed and synthesized from the
natural product myricitrin, which were structurally characterized by nuclear magnetic …

Palbociclib and Michael-acceptor hybrid compounds as CDK4/6 covalent inhibitors: Improved potency, broad anticancer spectrum and overcoming drug resistance

L Fang, M Chu, C Yan, Y Liu, Z Zhao - Bioorganic & medicinal chemistry, 2023 - Elsevier
To search for potent CDK4/6 covalent inhibitors, total 14 compounds have been designed
and synthesized by connecting different Michael-acceptor to the piperazine moiety of …

Pyridazinones: A versatile scaffold in the development of potential target‐based novel anticancer agents

J Singh, V Kumar, P Silakari… - Journal of Heterocyclic …, 2023 - Wiley Online Library
Pyridazinones are important nitrogen‐rich heterocyclic core that has been driving the
substantial medicinal interest due to their wide range of biological activities. This privileged …

Covalent inhibitors: An ambitious approach for the discovery of newer oncotherapeutics

RS Cheke, PS Kharkar - Drug Development Research, 2024 - Wiley Online Library
Covalent inhibitors have been used to treat several diseases for over a century. However,
strategic approaches for the rational design of covalent drugs have taken a definitive shape …

3D-QSAR, docking and molecular dynamics simulations of novel Pyrazolo-pyridazinone derivatives as covalent inhibitors of FGFR1: a scientific approach for possible …

S Hamza, A Abid, A Khanum, TA Chohan… - Journal of …, 2024 - Taylor & Francis
Developing highly potent covalent inhibitors of Fibroblast growth factor receptors 1 (FGFR1)
has always been a challenging task. In the current study, various computational techniques …

KinomeMETA: meta-learning enhanced kinome-wide polypharmacology profiling

Q Ren, N Qu, J Sun, J Zhou, J Liu, L Ni… - Briefings in …, 2024 - academic.oup.com
Kinase inhibitors are crucial in cancer treatment, but drug resistance and side effects hinder
the development of effective drugs. To address these challenges, it is essential to analyze …