Evidence map›Paper›PMID 34056161›Full record

ArticleACS omega2021

Design, Synthesis, Characterization, and Crystal Structure Studies of Nrf2 Modulators for Inhibiting Cancer Cell Growth In Vitro and In Vivo.

Prathima Chikkegowda, Baburajeev C Pookunoth, Venugopal R Bovilla, Prashanthkumar M Veeresh, Zonunsiami Leihang, Thippeswamy Thippeswamy, Mahesh A Padukudru, Basavanagowdappa Hathur, Rangappa S Kanchugarakoppal, Basappa and 1 more

Open access · goldAbstract read
In one paragraph

Article in ACS omega, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
0.6field-weighted citation impact, top 36% 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

6 citing papers in PubMed, 9 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Article
  5. Article
  6. Development of targeted therapy of NRF2Cellular signalling · 2021
    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 2 institutions in 1 country.

Prathima ChikkegowdaDepartment of Pharmacology, JSS Medical College, JSS Academy of Higher Education & Research, Mysore 570015, Karnataka, India.
Baburajeev C PookunothLaboratory of Chemical Biology, Department of Studies in Organic Chemistry, University of Mysore, Mysore 570005, Karnataka, India.
Venugopal R BovillaDepartment of Biochemistry (DST-FIST Supported Department), JSS Medical College, JSS Academy of Higher Education & Research, Mysore 570015, Karnataka, India.
Prashanthkumar M VeereshDepartment of Biochemistry (DST-FIST Supported Department), JSS Medical College, JSS Academy of Higher Education & Research, Mysore 570015, Karnataka, India.
Zonunsiami LeihangDepartment of Biochemistry (DST-FIST Supported Department), JSS Medical College, JSS Academy of Higher Education & Research, Mysore 570015, Karnataka, India.
Thippeswamy ThippeswamyDepartment of General Medicine, JSS Medical College and Hospital, JSS Academy of Higher Education & Research, Mysore 570015, Karnataka, India.
Mahesh A PadukudruDepartment of Respiratory Medicine, JSS Medical College, and Hospital, JSS Academy of Higher Education & Research, Mysore 570015, Karnataka, India.
Basavanagowdappa HathurCenter of Excellence in Molecular Biology and Regenerative Medicine (CEMR, DST-FIST Supported Center), JSS Medical College, JSS Academy of Higher Education & Research, Mysore 570015, Karnataka, India.
Rangappa S KanchugarakoppalDepartment of Studies in Chemistry, University of Mysore, Mysore 570005, Karnataka, India.
BasappaLaboratory of Chemical Biology, Department of Studies in Organic Chemistry, University of Mysore, Mysore 570005, Karnataka, India.ORCID 0000-0002-6810-9219
SubbaRao V MadhunapantulaDepartment of Biochemistry (DST-FIST Supported Department), JSS Medical College, JSS Academy of Higher Education & Research, Mysore 570015, Karnataka, India.ORCID 0000-0001-9167-9271
JSS Academy of Higher Education and Research · INUniversity of Mysore · IN

Funding

Research Mentoring and Building Capacity of underrepresented Minority Research Scientists in India.D43TW010540 · FIC · YALE UNIVERSITY · PI MICHELE BARRY, Eva Harris · 2017 to 2026
$15.5M
FIC NIH HHS D43 TW010540
6 · The paper itself

Abstract

Nrf2 is one of the important therapeutic targets studied extensively in several cancers including the carcinomas of the colon and rectum. However, to date, not many Nrf2 inhibitors showed promising results for retarding the growth of colorectal cancers (CRCs). Therefore, in this study, first, we have demonstrated the therapeutic effect of siRNA-mediated downmodulation of Nrf2 on the proliferation rate of CRC cell lines. Next, we have designed, synthesized, characterized, and determined the crystal structures for a series of tetrahydrocarbazoles (THCs) and assessed their potential to modulate the activity of Nrf2 target gene NAD(P)H:quinone oxidoreductase (NQO1) activity by treating colorectal carcinoma cell line HCT-116. Later, the cytotoxic potential of compounds was assessed against cell lines expressing varying amounts of Nrf2, viz., breast cancer cell lines MDA-MB-231 and T47D (low functionally active Nrf2), HCT-116 (moderately active Nrf2), and lung cancer cell line A549 (highly active Nrf2), and the lead compound

Identifiers

PMID34056161
PMCPMC8153663
OpenAlexW3156865326

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.