Biologically active quinazoline-based hydroxamic acids
Sign Up to like & getrecommendations! Published in 2020 at "Medicinal Chemistry Research"
DOI: 10.1007/s00044-020-02530-7
Abstract: Molecular hybridization has become a new promising way to treat multifactorial diseases with a single compound that acts on multiple targets. The combination of several functional pharmacophore groups in one molecule can lead to a… read more here.
Keywords: based hydroxamic; quinazoline based; active quinazoline; chemistry ... See more keywords
Macrocyclization of Quinazoline-Based EGFR Inhibitors Leads to Exclusive Mutant Selectivity for EGFR L858R and Del19.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01041
Abstract: Activating mutations in the epidermal growth factor receptor (EGFR) are frequent oncogenic drivers of non-small-cell lung cancer (NSCLC). The most frequent alterations in EGFR are short in-frame deletions in exon 19 (Del19) and the missense… read more here.
Keywords: macrocyclization quinazoline; based egfr; egfr inhibitors; quinazoline ... See more keywords
Quinazoline-based human phosphodiesterase 5 inhibitors exhibited a selective vasorelaxant effect on rat isolated pulmonary arteries involving NO-sGC-cGMP pathway and calcium inhibitory effects.
Sign Up to like & getrecommendations! Published in 2022 at "Vascular pharmacology"
DOI: 10.2139/ssrn.4197599
Abstract: Phosphodiesterase 5 (PDE5) inhibitors are an attractive option among the currently available therapies in the management of pulmonary arterial hypertension (PAH). Good selectivity for PDE5 is associated with reduced side effects and greater vasorelaxant effect… read more here.
Keywords: vasorelaxant effect; rat isolated; effect; quinazoline based ... See more keywords
Quinazoline Based HDAC Dual Inhibitors as Potential Anti-Cancer Agents
Sign Up to like & getrecommendations! Published in 2022 at "Molecules"
DOI: 10.3390/molecules27072294
Abstract: Cancer is the most devastating disease and second leading cause of death around the world. Despite scientific advancements in the diagnosis and treatment of cancer which can include targeted therapy, chemotherapy, endocrine therapy, immunotherapy, radiotherapy… read more here.
Keywords: cancer; dual inhibitors; anti cancer; quinazoline based ... See more keywords
Some novel hybrid quinazoline-based heterocycles as potent cytotoxic agents
Sign Up to like & getrecommendations! Published in 2022 at "Research in Pharmaceutical Sciences"
DOI: 10.4103/1735-5362.329923
Abstract: Background and purpose: In this study, some new cytotoxic hybrid structures were synthesized by combining pyrazolinone and imidazolinone rings with quinazoline pharmacophores. Experimental approach: The benzoxazinone, pyrazolo-quinazoline fused ring, and imidazolinone anchored quinazoline derivatives were… read more here.
Keywords: cytotoxic; cell line; quinazoline based; quinazoline ... See more keywords
Quinazoline-based analog of adenine as an antidote against MLL-rearranged leukemia cells: synthesis, inhibition assays and docking studies.
Sign Up to like & getrecommendations! Published in 2022 at "Future medicinal chemistry"
DOI: 10.4155/fmc-2021-0251
Abstract: Background: Post-translational modifications of histones constitute a dynamic process impacting gene expression. A well-studied modification is lysine methylation. Among the lysine histone methyltransferases, DOT1L is implicated in various diseases, making it a very interesting target… read more here.
Keywords: based analog; adenine antidote; mll rearranged; antidote mll ... See more keywords