Evidence map›Paper›PMID 35178174›Full record

ArticleACS medicinal chemistry letters2022

Design, Synthesis, and Biological Evaluation of Apcin-Based CDC20 Inhibitors.

Rajib Bhuniya, Xinrui Yuan, Longchuan Bai, Kathryn L Howie, Rui Wang, Wei Li, Frank Park, Chao-Yie Yang

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2022. 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
1.2field-weighted citation impact, top 23% 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, 14 citations in OpenAlex.

  1. The Use of APC/C Antagonists to Promote Mitotic Catastrophe in Cancer Cells.Methods in molecular biology (Clifton, N.J.) · 2025
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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

8 authors at 2 institutions in 1 country.

Rajib BhuniyaDepartments of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Xinrui YuanDepartments of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Longchuan BaiDepartment of Internal Medicine, Hematology & Oncology Division, University of Michigan, Ann Arbor, Michigan 48109, United States.
Kathryn L HowieDepartments of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Rui WangDepartments of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.ORCID https://orcid.org/0000-0001-9348-1058
Wei LiDepartments of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.ORCID https://orcid.org/0000-0002-9522-4474
Frank ParkDepartments of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.
Chao-Yie YangDepartments of Pharmaceutical Sciences, College of Pharmacy, University of Tennessee Health Science Center, Memphis, Tennessee 38163, United States.ORCID https://orcid.org/0000-0002-5445-0109
University of Tennessee Health Science Center · USUniversity of Michigan · US

Funding

Targeting the colchicine site in tubulin for advanced melanomaR01CA148706 · NCI · UNIVERSITY OF TENNESSEE HEALTH SCI CTR · PI LI, WEI, MILLER, DUANE D · 2011 to 2025
$5.3M
NCI NIH HHS R01 CA148706
6 · The paper itself

Abstract

CDC20 binds to anaphase-promoting complex/cyclosome E3 ubiquitin ligase to recruit substrates for ubiquitination to promote mitotic progression. In breast and other cancers, CDC20 overexpression causes cell cycle dysregulation and is associated with poor prognosis. Apcin was previously discovered as a CDC20 inhibitor exhibiting high micromolar activities. Here, we designed and developed new apcin-based inhibitors by eliminating a controlled substance, chloral hydrate, required for synthesis. We further improved the antitumor activities of the inhibitors by replacing the pyrimidine group with substituted thiazole-containing groups. When evaluated in MDA-MB-231 and MDA-MB-468 triple negative breast cancer cell lines, several analogs showed 5-10-fold improvement over apcin with IC

Identifiers

PMID35178174
PMCPMC8842116
OpenAlexW4206059486

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.