Evidence map›Paper›PMID 20064715›Full record

ArticleBioorganic & medicinal chemistry letters2010

3,5-Bis(benzylidene)-1-[4-2-(morpholin-4-yl)ethoxyphenylcarbonyl]-4-piperidone hydrochloride: a lead tumor-specific cytotoxin which induces apoptosis and autophagy.

Umashankar Das, Hiroshi Sakagami, Qing Chu, Qintao Wang, Masami Kawase, Ponniah Selvakumar, Rajendra K Sharma, Jonathan R Dimmock

Open access · greenAbstract readComparative Study
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2010. 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
2.0field-weighted citation impact, top 14% 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, 42 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Article
  5. 1-Benzyl-3,5-bis-(4-methyl-benzyl-idene)-4-oxopiperidin-1-ium chloride acetic acid monosolvate.Acta crystallographica. Section E, Structure reports online · 2011
    Article
  6. 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

8 authors at 4 institutions in 3 countries.

Umashankar DasDrug Design and Discovery Research Group, College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, Saskatchewan, Canada S7N 5C9.
Hiroshi Sakagami
Qing Chu
Qintao Wang
Masami Kawase
Ponniah Selvakumar
Rajendra K Sharma
Jonathan R Dimmock
University of Saskatchewan · CAAir Force Medical University · CNMatsuyama University · JPMeikai University · JP

Funding

CIHR 53171
6 · The paper itself

Abstract

A number of N-4-(2-aminoethoxy)phenylcarbonyl derivatives of various 3,5-bis(benzylidene)-4-piperidones 2-5 demonstrated noteworthy cytotoxic potencies towards human HL-60 leukemic cells as well as human HSC-2 and HSC-4 squamous cell carcinomas. In general, toxicity towards HGF, HPC, and HPLF normal cells was substantially lower. The highest selective toxicity was noted when the terminal base is morpholine. Lead optimization was based on finding compounds which had (i) high cytotoxic potencies, (ii) a greater toxicity to neoplasms than normal cells, and (iii) drug-likeness based on the rule of five. From the biodata generated, 5a evolved as a promising lead compound for further development. The mode of action of 5a included the induction of apoptosis in HL-60 cells in which internucleosomal DNA fragmentation and activation of caspase-3 was noted. In addition, 5a caused autophagy in HSC-2 cells.

Indexed as

Quantitative Structure-Activity RelationshipAntineoplastic AgentsApoptosisAutophagyCell Line, TumorCytotoxinsDrug Screening Assays, AntitumorHL-60 CellsHT29 CellsHumansPiperidones3,5-bis(benzylidene)-4-piperidoneAntineoplastic AgentsCytotoxinsPiperidones

Identifiers

PMID20064715
PMCPMC3276597
OpenAlexW2063593425

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.