Evidence map›Paper›PMID 33869816›Full record

ArticleHeliyon2021

Design, synthesis and evaluation of novel enzalutamide analogues as potential anticancer agents.

Ritesh P Bhole, Rupesh V Chikhale, Ravindra D Wavhale, Fatmah Ali Asmary, Tahani Mazyad Almutairi, Hassna Mohammed Alhajri, Chandrakant G Bonde

Abstract read
In one paragraph

Article in Heliyon, 2021. 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
–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

5 citing papers in PubMed.

  1. Article
  2. Review
  3. Article
  4. Article
  5. 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

7 authors.

Ritesh P BholeDr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune 411018, Maharashtra, India.
Rupesh V ChikhaleDivision of Pharmacy and Optometry, University of Manchester, Manchester, UK.
Ravindra D WavhaleDr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune 411018, Maharashtra, India.
Fatmah Ali AsmaryDepartment of Chemistry, P.O. Box 2455, College of Science, King Saud University, Riyadh, 11451, Saudi Arabia.
Tahani Mazyad AlmutairiDepartment of Chemistry, P.O. Box 2455, College of Science, King Saud University, Riyadh, 11451, Saudi Arabia.
Hassna Mohammed AlhajriDepartment of Chemistry, P.O. Box 2455, College of Science, King Saud University, Riyadh, 11451, Saudi Arabia.
Chandrakant G BondeSchool of Pharmacy & Technology Management, SVKM's NarseeMonjee Institute of Management & Studies (NMIMS), Mukesh Patel Technology Park, Shirpur, Dhule, 425405, Maharashtra, India.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The androgen receptor inhibitor, Enzalutamide, proved effective against castration resistance prostate cancer, has demonstrated clinical benefits and increased survival rate in men. However, AR mutation (F876L) converts Enzalutamide from antagonist to agonist indicating a rapid evolution of resistance. Hence, our goal is to overcome this resistance mechanism by designing and developing novel Enzalutamide analogues. We designed a dataset of Enzalutamide derivatives using Enzalutamide's shape and electrostatic features to match with pharmacophoric features essential for tight binding with the androgen receptor. Based on this design strategy ten novel derivatives were selected including 5,5-dimethyl-3-(6-substituted benzo[d]thia/oxazol-2-yl)-2-thioxo-1-(4-(trifluoromethyl)pyridin-2-yl)imidazolidin-4-one (

Indexed as

Binding energy calculationsHybrid moleculesImidazolidinone derivativesMolecular dockingMolecular dynamics simulationsProstate cancer

Identifiers

PMID33869816
PMCPMC8035491

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.