Evidence map›Paper›PMID 35909144›Full record

ArticleMolecular diversity2023

Identification of bicyclic compounds that act as dual inhibitors of Bcl-2 and Mcl-1.

Abhay Uthale, Aarti Anantram, Prasad Sulkshane, Mariam Degani, Tanuja Teni

Abstract read
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In one paragraph

Article in Molecular diversity, 2023. 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
0.4field-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, 6 citations in OpenAlex.

  1. Review
  2. 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

5 authors at 2 institutions in 1 country.

Abhay Uthale *Advanced Centre for Treatment, Research & Education in Cancer (ACTREC), Tata Memorial Centre, Kharghar, Navi Mumbai, 410 210, India.ORCID http://orcid.org/0000-0003-2152-9539
Aarti Anantram *Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Mumbai, 400 019, India.ORCID http://orcid.org/0000-0001-5855-8128
Prasad SulkshaneAdvanced Centre for Treatment, Research & Education in Cancer (ACTREC), Tata Memorial Centre, Kharghar, Navi Mumbai, 410 210, India.ORCID http://orcid.org/0000-0002-5517-1355
Mariam DeganiDepartment of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Mumbai, 400 019, India. ms.degani@ictmumbai.edu.in.ORCID http://orcid.org/0000-0002-3455-2642
Tanuja TeniAdvanced Centre for Treatment, Research & Education in Cancer (ACTREC), Tata Memorial Centre, Kharghar, Navi Mumbai, 410 210, India. tteni@actrec.gov.in.ORCID http://orcid.org/0000-0003-3229-4296
Homi Bhabha National Institute · INInstitute of Chemical Technology · IN

Funding

TEQIP Grant TEQIP II/TEQIP-II/MH/MH2G01/386/347
6 · The paper itself

Abstract

Elevated expression of anti-apoptotic proteins, such as Bcl-2 and Mcl-1 contributes to poor prognosis and resistance to current treatment modalities in multiple cancers. Here, we report the design, synthesis and characterization of benzimidazole chalcone and flavonoid scaffold-derived bicyclic compounds targeting both Bcl-2 and Mcl-1 by optimizing the structural differences in the binding sites of both these proteins. Initial docking screen of Bcl-2 and Mcl-1 with pro-apoptotic protein Bim revealed possible hits with optimal binding energies. All the optimized bicyclic compounds were screened for their in vitro cytotoxic activity against two oral cancer cell lines (AW8507 and AW13516) which express high levels of Bcl-2 and Mcl-1. Compound 4d from the benzimidazole chalcone series and compound 6d from the flavonoid series exhibited significant cytotoxic activity (IC

Indexed as

ChalconesMouth NeoplasmsApoptosisApoptosis Regulatory Proteinsbcl-2 Homologous Antagonist-Killer Proteinbcl-X ProteinBenzimidazolesBridged Bicyclo CompoundsCell Line, TumorHumansApoptosis Regulatory Proteinsbcl-2 Homologous Antagonist-Killer Proteinbcl-X ProteinBenzimidazolesBridged Bicyclo CompoundsChalconesApoptosisBcl-2BenzimidazolesFlavonoidsMcl-1TR-FRET assay

Identifiers

PMID35909144
OpenAlexW4289318113

What OpenQuestion 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 OpenQuestion graph.