Evidence map›Paper›PMID 35978701›Full record

ArticleACS medicinal chemistry letters2022

Quinolines and Oxazino-quinoline Derivatives as Small Molecule GLI1 Inhibitors Identified by Virtual Screening.

Fabrizio Manetti, Luisa Maresca, Enrica Crivaro, Sara Pepe, Elena Cini, Snigdha Singh, Paolo Governa, Samuele Maramai, Giuseppe Giannini, Barbara Stecca and 1 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.7field-weighted citation impact, top 33% 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

5 citing papers in PubMed, 8 citations in OpenAlex.

  1. Review
  2. Review
  3. Article
  4. Review
  5. Emerging Roles of Hedgehog Signaling in Cancer Immunity.International journal of molecular sciences · 2023
    Review
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

11 authors at 3 institutions in 1 country.

Fabrizio ManettiDipartimento di Biotecnologie Chimica e Farmacia, Università di Siena, via A. Moro 2, I-53100 Siena, Italy.ORCID https://orcid.org/0000-0002-9598-2339
Luisa MarescaIstituto per lo Studio, la Prevenzione e la Rete Oncologica (ISPRO), Viale Pieraccini 6, I-50139 Firenze, Italy.
Enrica CrivaroIstituto per lo Studio, la Prevenzione e la Rete Oncologica (ISPRO), Viale Pieraccini 6, I-50139 Firenze, Italy.ORCID https://orcid.org/0000-0002-6098-3315
Sara PepeIstituto per lo Studio, la Prevenzione e la Rete Oncologica (ISPRO), Viale Pieraccini 6, I-50139 Firenze, Italy.
Elena CiniDipartimento di Biotecnologie Chimica e Farmacia, Università di Siena, via A. Moro 2, I-53100 Siena, Italy.ORCID https://orcid.org/0000-0003-4420-8930
Snigdha SinghDipartimento di Biotecnologie Chimica e Farmacia, Università di Siena, via A. Moro 2, I-53100 Siena, Italy.
Paolo GovernaDipartimento di Biotecnologie Chimica e Farmacia, Università di Siena, via A. Moro 2, I-53100 Siena, Italy.ORCID https://orcid.org/0000-0002-5976-780X
Samuele MaramaiDipartimento di Biotecnologie Chimica e Farmacia, Università di Siena, via A. Moro 2, I-53100 Siena, Italy.ORCID https://orcid.org/0000-0001-7499-6961
Giuseppe GianniniR&D, Alfasigma SpA, I-00071 Pomezia (Roma), Italy.ORCID https://orcid.org/0000-0002-7127-985X
Barbara SteccaIstituto per lo Studio, la Prevenzione e la Rete Oncologica (ISPRO), Viale Pieraccini 6, I-50139 Firenze, Italy.ORCID https://orcid.org/0000-0003-1197-1622
Elena PetricciDipartimento di Biotecnologie Chimica e Farmacia, Università di Siena, via A. Moro 2, I-53100 Siena, Italy.
University of Siena · ITIstituto per lo Studio e la Prevenzione Oncologica · ITAlfasigma (Italy) · IT

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A virtual screening approach based on a five-feature pharmacophoric model for negative modulators of GLI1 was applied to databases of commercially available compounds. The resulting quinoline derivatives showed significant ability to reduce the GLI1 protein level and were characterized by submicromolar antiproliferative activity toward human melanoma A375 and medulloblastoma DAOY cell lines. Decoration of the quinoline ring and chemical rigidification to an oxazino-quinoline scaffold allowed us to deduce SAR considerations for future ligand optimization.

Identifiers

PMID35978701
PMCPMC9377010
OpenAlexW4286560485

What Socratic holds

Textmetadata
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 Socratic graph.