Evidence map›Paper›PMID 37849704›Full record

ArticleRSC advances2023

Design, synthesis and biological evaluation of tetrahydroquinoxaline sulfonamide derivatives as colchicine binding site inhibitors.

Haiyang Dong, Lu Lu, Xueting Song, Youkang Li, Jinguang Zhou, Yungen Xu, Yahong Zhang, Jianguo Qi, Tingting Liang, Jianhong Wang

Abstract read
In one paragraph

Article in RSC advances, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing 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

3 citing papers in PubMed.

  1. Review
  2. Review
  3. Article
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

10 authors.

Haiyang DongKey Laboratory of Natural Medicine and Immune-Engineering of Henan Province, Henan University Jinming Campus Kaifeng 475004 Henan China liangting910710@126.com.
Lu LuKey Laboratory of Natural Medicine and Immune-Engineering of Henan Province, Henan University Jinming Campus Kaifeng 475004 Henan China liangting910710@126.com.
Xueting SongKey Laboratory of Natural Medicine and Immune-Engineering of Henan Province, Henan University Jinming Campus Kaifeng 475004 Henan China liangting910710@126.com.
Youkang LiKey Laboratory of Natural Medicine and Immune-Engineering of Henan Province, Henan University Jinming Campus Kaifeng 475004 Henan China liangting910710@126.com.
Jinguang ZhouHuaihe Hospital of Henan University Kaifeng 475004 Henan China.
Yungen XuDepartment of Medicinal Chemistry, Jiangsu Key Laboratory of Drug Design and Optimization, China Pharmaceutical University Nanjing 211198 China.
Yahong ZhangKey Laboratory of Natural Medicine and Immune-Engineering of Henan Province, Henan University Jinming Campus Kaifeng 475004 Henan China liangting910710@126.com.
Jianguo QiKey Laboratory of Natural Medicine and Immune-Engineering of Henan Province, Henan University Jinming Campus Kaifeng 475004 Henan China liangting910710@126.com.
Tingting LiangKey Laboratory of Natural Medicine and Immune-Engineering of Henan Province, Henan University Jinming Campus Kaifeng 475004 Henan China liangting910710@126.com.ORCID https://orcid.org/0000-0001-5291-0995
Jianhong WangKey Laboratory of Natural Medicine and Immune-Engineering of Henan Province, Henan University Jinming Campus Kaifeng 475004 Henan China liangting910710@126.com.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Colchicine binding site inhibitors (CBSIs) are potential microtubule targeting agents (MTAs), which can overcome multidrug resistance, improve aqueous solubility and reduce toxicity faced by most MTAs. Novel tetrahydroquinoxaline sulfonamide derivatives were designed, synthesized and evaluated for their antiproliferative activities. The MTT assay results demonstrated that some derivatives exhibited moderate to strong inhibitory activities against HT-29 cell line. Among them, compound I-7 was the most active compound. Moreover, I-7 inhibited tubulin polymerization, disturbed microtubule network, disrupted the formation of mitotic spindle and arrested cell cycle at G2/M phase. However, I-7 didn't induce cell apoptosis. Furthermore, the prediction of ADME demonstrated that I-7 showed favorable physiochemical and pharmacokinetic properties. And the detailed molecular docking confirmed I-7 targeted the site of colchicine through hydrogen and hydrophobic interactions.

Identifiers

PMID37849704
PMCPMC10577396

What Socratic holds

Textmetadata
LicenceCC BY-NC
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 Socratic graph.