Synthesis and Biological Evaluation of 2-Substituted Benzyl-/Phenylethylamino-4-amino-5-aroylthiazoles as Apoptosis-Inducing Anticancer Agents.
Paola Oliva, Valentina Onnis, Elisa Balboni, Ernest Hamel, Francisco Estévez-Sarmiento, José Quintana, Francisco Estévez, Andrea Brancale, Salvatore Ferla, Stefano Manfredini and 1 more
Article in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.5field-weighted citation impact, top 41% of its field
1 · What the graph read from it
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
2 · The registry
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
3 · Its place in the literature
Who cites it
2 citing papers in PubMed, 8 citations in OpenAlex.
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
5 · Who and what money
Authors and funding
11 authors at 5 institutions in 4 countries.
Paola OlivaDipartimento di Scienze Chimiche e Farmaceutiche, University of Ferrara, Via L. Borsari 46, 44121 Ferrara, Italy.
Valentina OnnisDipartimento di Scienze della Vita e dell'Ambiente, University of Cagliari, University Campus, 09042 Monserrato (Cagliari), Italy.ORCID 0000-0002-2438-725X
Elisa BalboniDipartimento di Scienze Chimiche e Farmaceutiche, University of Ferrara, Via L. Borsari 46, 44121 Ferrara, Italy.
Ernest HamelScreening Technologies Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, Frederick National Laboratory for Cancer Research, National Cancer Institute, National Institute of Health, Frederick, MD 21702, USA.
Francisco Estévez-SarmientoDepartamento de Bioquímica y Biología Molecular, Instituto Universitario de Investigaciones Biomédicas y Sanitarias, Universidad de las Palmas de Gran Canaria, E-35016 Las Palmas de Gran Canaria, Spain.
José QuintanaDepartamento de Bioquímica y Biología Molecular, Instituto Universitario de Investigaciones Biomédicas y Sanitarias, Universidad de las Palmas de Gran Canaria, E-35016 Las Palmas de Gran Canaria, Spain.ORCID 0000-0001-8225-4538
Francisco EstévezDepartamento de Bioquímica y Biología Molecular, Instituto Universitario de Investigaciones Biomédicas y Sanitarias, Universidad de las Palmas de Gran Canaria, E-35016 Las Palmas de Gran Canaria, Spain.
Andrea BrancaleSchool of Pharmacy and Pharmaceutical Sciences, Cardiff University, King Edward VII Avenue, Cardiff CF10 3NB, UK.
Salvatore FerlaSchool of Pharmacy and Pharmaceutical Sciences, Cardiff University, King Edward VII Avenue, Cardiff CF10 3NB, UK.
Stefano ManfrediniDipartimento di Scienze della Vita e Biotecnologie, Università di Ferrara, 44121 Ferrara, Italy.ORCID 0000-0003-1348-4422
Romeo RomagnoliDipartimento di Scienze Chimiche e Farmaceutiche, University of Ferrara, Via L. Borsari 46, 44121 Ferrara, Italy.ORCID 0000-0002-6374-773X
University of Ferrara · ITUniversidad de Las Palmas de Gran Canaria · ESCardiff University · GBFrederick National Laboratory for Cancer Research · USUniversity of Cagliari · IT
Funding
European Regional Development Fund through the Welsh Government Sêr Cymru programmeMinistero dell'Istruzione, dell'Università e della Ricerca PRIN 2017 grant 2017E84AA4_002
6 · The paper itself
Abstract
Induction of apoptosis is a common chemotherapeutic mechanism to kill cancer cells The thiazole system has been reported over the past decades as a building block for the preparation of anticancer agents. A novel series of 2-arylalkylamino-4-amino-5-(3',4',5'-trimethoxybenzoyl)-thiazole derivatives designed as dual inhibitors of tubulin and cyclin-dependent kinases (CDKs) were synthesized and evaluated for their antiproliferative activity in vitro against two cancer cell lines and, for selected highly active compounds, for interactions with tubulin and cyclin-dependent kinases and for cell cycle and apoptosis effects. Structure-activity relationships were elucidated for various substituents at the 2-position of the thiazole skeleton. Among the synthesized compounds, the most active analogues were found to be the
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.
Synthesis and Biological Evaluation of 2-Substituted Benzyl-/Phenylethylamino-4-amino-5-aroylthiazoles as Apoptosis-Inducing Anticancer Agents. · full record | OpenQuestion