Evidence map›Paper›PMID 35745866›Full record

ArticlePharmaceutics2022

Design, Synthesis, In Silico Studies and Inhibitory Activity towards Bcr-Abl, BTK and FLT3-ITD of New 2,6,9-Trisubstituted Purine Derivatives as Potential Agents for the Treatment of Leukaemia.

Jeanluc Bertrand, Hana Dostálová, Vladimír Kryštof, Radek Jorda, Thalía Delgado, Alejandro Castro-Alvarez, Jaime Mella, David Cabezas, Mario Faúndez, Christian Espinosa-Bustos and 1 more

Abstract read
In one paragraph

Article in Pharmaceutics, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
–field-weighted citation impact
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

8 citing papers in PubMed.

  1. Review
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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.

Jeanluc BertrandDepartamento de Química Orgánica, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Avenida Vicuña Mackenna 4860, Santiago 7820436, Chile.
Hana DostálováDepartment of Experimental Biology, Palacký University Olomouc, Šlechtitelů 27, 783 71 Olomouc, Czech Republic.ORCID 0000-0002-6123-6450
Vladimír KryštofDepartment of Experimental Biology, Palacký University Olomouc, Šlechtitelů 27, 783 71 Olomouc, Czech Republic.ORCID 0000-0001-5838-2118
Radek JordaDepartment of Experimental Biology, Palacký University Olomouc, Šlechtitelů 27, 783 71 Olomouc, Czech Republic.ORCID 0000-0002-4905-7126
Thalía DelgadoDepartamento de Química Orgánica, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Avenida Vicuña Mackenna 4860, Santiago 7820436, Chile.
Alejandro Castro-AlvarezDepartamento de Ciencias Preclínicas, Facultad de Medicina, Universidad de La Frontera, Manuel Montt 112, Temuco 4780000, Chile.ORCID 0000-0001-8360-8027
Jaime MellaInstituto de Química y Bioquímica, Facultad de Ciencias, Universidad de Valparaíso, Avenida Gran Bretaña 1111, Valparaíso 2360102, Chile.ORCID 0000-0002-2434-8461
David CabezasInstituto de Química y Bioquímica, Facultad de Ciencias, Universidad de Valparaíso, Avenida Gran Bretaña 1111, Valparaíso 2360102, Chile.
Mario FaúndezDepartamento de Farmacia, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Avenida Vicuña Mackenna 4860, Santiago 7820436, Chile.
Christian Espinosa-BustosDepartamento de Farmacia, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Avenida Vicuña Mackenna 4860, Santiago 7820436, Chile.ORCID 0000-0001-6038-8439
Cristian O SalasDepartamento de Química Orgánica, Facultad de Química y de Farmacia, Pontificia Universidad Católica de Chile, Avenida Vicuña Mackenna 4860, Santiago 7820436, Chile.ORCID 0000-0001-7620-2459

Funding

Conicyt, Chile Nº21180975.Czech Science Foundation 21-06553SEuropean Regional Development Fund ENOCH, No. CZ.02.1.01/0.0/0.0/16_019/0000868Palacký University, Olomouc IGA_PrF_2022_007
6 · The paper itself

Abstract

We report 31 new compounds designed, synthesized and evaluated on Bcr-Abl, BTK and FLT3-ITD as part of our program to develop 2,6,9-trisubstituted purine derivatives as inhibitors of oncogenic kinases. The design was inspired by the chemical structures of well-known kinase inhibitors and our previously developed purine derivatives. The synthesis of these purines was simple and used a microwave reactor for the final step. Kinase assays showed three inhibitors with high selectivity for each protein that were identified:

Indexed as

3D-QSARleukaemiamolecular dockingpurine derivativestyrosine kinases inhibitors

Identifiers

PMID35745866
PMCPMC9228270

What OpenQuestion holds

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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.