Evidence map›Paper›PMID 29259754›Full record

ArticleACS medicinal chemistry letters2017

Discovery of New Sulfonamide Carbonic Anhydrase IX Inhibitors Incorporating Nitrogenous Bases.

Alessio Nocentini, Silvia Bua, Carrie L Lomelino, Robert McKenna, Marta Menicatti, Gianluca Bartolucci, Barbara Tenci, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Paola Gratteri and 1 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
4.1field-weighted citation impact, top 5% 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

16 citing papers in PubMed, 76 citations in OpenAlex.

  1. Article
  2. Drug Design of Carbonic Anhydrase Inhibitors.Sub-cellular biochemistry · 2026
    Review
  3. Article
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  5. Isocoumarins: a new class of selective carbonic anhydrase IX and XII inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2022
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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 2 institutions in 2 countries.

Alessio NocentiniDepartment of NEUROFARBA, Pharmaceutical and Nutraceutical section, University of Florence, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
Silvia BuaDepartment of NEUROFARBA, Pharmaceutical and Nutraceutical section, University of Florence, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
Carrie L LomelinoDepartment of Biochemistry and Molecular Biology, College of Medicine, University of Florida, Box 100245, Gainesville, Florida 32610, United States.
Robert McKennaDepartment of Biochemistry and Molecular Biology, College of Medicine, University of Florida, Box 100245, Gainesville, Florida 32610, United States.
Marta MenicattiDepartment of NEUROFARBA, Pharmaceutical and Nutraceutical section, University of Florence, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
Gianluca BartolucciDepartment of NEUROFARBA, Pharmaceutical and Nutraceutical section, University of Florence, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
Barbara TenciDepartment of NEUROFARBA-Pharmacology and Toxicology Section, University of Florence, Viale G. Pieraccini 6, 50019 Florence, Italy.
Lorenzo Di Cesare MannelliDepartment of NEUROFARBA-Pharmacology and Toxicology Section, University of Florence, Viale G. Pieraccini 6, 50019 Florence, Italy.
Carla GhelardiniDepartment of NEUROFARBA-Pharmacology and Toxicology Section, University of Florence, Viale G. Pieraccini 6, 50019 Florence, Italy.
Paola GratteriDepartment of NEUROFARBA, Pharmaceutical and Nutraceutical section, University of Florence, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
Claudiu T SupuranDepartment of NEUROFARBA, Pharmaceutical and Nutraceutical section, University of Florence, Via Ugo Schiff 6, Sesto Fiorentino, 50019 Florence, Italy.
University of Florence · ITUniversity of Florida · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Incorporation of the purine/pyrimidine moieties as tails to classical benzenesulfonamide scaffolds afforded two series of human (h) carbonic anhydrase (CA, EC 4.2.1.1) inhibitors. The compounds were designed according to the molecular hybridization approach, in order to modulate the interaction with different CA isozymes and exploit the antitumor effect of uracil and adenine derivatives in parallel and synergic mode to the inhibition of the tumor-associated hCA IX. The sulfonamides were investigated as inhibitors of four isoforms, cytosolic hCA I/II and transmembrane hCA IV/IX. The inhibitory profiles were dependent on the length and positioning of the spacer connecting the two pharmacophores. X-ray crystallography demonstrated the binding mode of an inhibitor to hCA II and hCA IX-mimic. Compounds endowed with the best hCA IX inhibitory efficacy were evaluated for antiproliferative activity against HT-29 colon cancer cell lines. The

Identifiers

PMID29259754
PMCPMC5733260
OpenAlexW2770193087

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Registered trials

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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.