Evidence map›Paper›PMID 38611732›Full record

ArticleMolecules (Basel, Switzerland)2024

Serendipitous Identification of Azine Anticancer Agents Using a Privileged Scaffold Morphing Strategy.

Silvia Cesarini, Ilaria Vicenti, Federica Poggialini, Silvia Filippi, Eleonora Mancin, Lia Fiaschi, Elisa De Marchi, Federica Giammarino, Chiara Vagaggini, Bruno Mattia Bizzarri and 4 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.5field-weighted citation impact, top 43% 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

1 citing paper in PubMed, 2 citations in OpenAlex.

  1. Article
4 · The record

Corrections and comments

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

14 authors at 2 institutions in 1 country.

Silvia CesariniDepartment of Biological and Ecological Sciences, University of Viterbo, Via S.C. De Lellis s.n.c., 01100 Viterbo, Italy.
Ilaria VicentiDepartment of Medical Biotechnologies, University of Siena, 53100 Siena, Italy.ORCID 0000-0002-4306-2960
Federica PoggialiniDepartment of Biotechnology, Chemistry, and Pharmacy (DBCF), University of Siena, 53100 Siena, Italy.ORCID 0000-0002-8225-4631
Silvia FilippiDepartment of Biological and Ecological Sciences, University of Viterbo, Via S.C. De Lellis s.n.c., 01100 Viterbo, Italy.ORCID 0000-0001-6213-7350
Eleonora MancinDepartment of Biological and Ecological Sciences, University of Viterbo, Via S.C. De Lellis s.n.c., 01100 Viterbo, Italy.
Lia FiaschiDepartment of Medical Biotechnologies, University of Siena, 53100 Siena, Italy.
Elisa De MarchiDepartment of Biological and Ecological Sciences, University of Viterbo, Via S.C. De Lellis s.n.c., 01100 Viterbo, Italy.ORCID 0000-0001-6116-9772
Federica GiammarinoDepartment of Medical Biotechnologies, University of Siena, 53100 Siena, Italy.ORCID 0000-0001-6775-3574
Chiara VagagginiDepartment of Biotechnology, Chemistry, and Pharmacy (DBCF), University of Siena, 53100 Siena, Italy.ORCID 0000-0002-4208-7760
Bruno Mattia BizzarriDepartment of Biological and Ecological Sciences, University of Viterbo, Via S.C. De Lellis s.n.c., 01100 Viterbo, Italy.ORCID 0000-0001-7085-5432
Raffaele SaladinoDepartment of Biological and Ecological Sciences, University of Viterbo, Via S.C. De Lellis s.n.c., 01100 Viterbo, Italy.ORCID 0000-0002-4420-9063
Elena DreassiDepartment of Biotechnology, Chemistry, and Pharmacy (DBCF), University of Siena, 53100 Siena, Italy.ORCID 0000-0001-8987-940X
Maurizio ZazziDepartment of Medical Biotechnologies, University of Siena, 53100 Siena, Italy.ORCID 0000-0002-0344-6281
Lorenzo BottaDepartment of Biological and Ecological Sciences, University of Viterbo, Via S.C. De Lellis s.n.c., 01100 Viterbo, Italy.ORCID 0000-0002-0856-2986
Università degli Studi della Tuscia · ITUniversity of Siena · IT

Funding

Ministry of Education, Universities and Research 2017BMK8JR
6 · The paper itself

Abstract

The use of privileged scaffolds as a starting point for the construction of libraries of bioactive compounds is a widely used strategy in drug discovery and development. Scaffold decoration, morphing and hopping are additional techniques that enable the modification of the chosen privileged framework and better explore the chemical space around it. In this study, two series of highly functionalized pyrimidine and pyridine derivatives were synthesized using a scaffold morphing approach consisting of triazine compounds obtained previously as antiviral agents. Newly synthesized azines were evaluated against lymphoma, hepatocarcinoma, and colon epithelial carcinoma cells, showing in five cases acceptable to good anticancer activity associated with low cytotoxicity on healthy fibroblasts. Finally, ADME in vitro studies were conducted on the best derivatives of the two series showing good passive permeability and resistance to metabolic degradation.

Indexed as

Antineoplastic AgentsCarcinoma, HepatocellularLiver NeoplasmsAntiviral AgentsAzo CompoundsHumansAntineoplastic AgentsAntiviral AgentsAzo Compoundsanticancer activityprivileged scaffoldpyridinespyrimidinesscaffold morphingtriazines

Identifiers

PMID38611732
PMCPMC11013010
OpenAlexW4393162721

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

Registered trials

None linked

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.