Evidence map›Paper›PMID 37196868›Full record

ArticleBioorganic & medicinal chemistry letters2023

Structure-activity relationship of BMS906024 derivatives for Cryptosporidium parvum growth inhibition.

Seungheon Lee, Melissa S Love, Ramkumar Modukuri, Arnab K Chatterjee, Lauren Huerta, Ann P Lawson, Case W McNamara, Jan R Mead, Lizbeth Hedstrom, Gregory D Cuny

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.6field-weighted citation impact, top 38% 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

2 citing papers in PubMed, 2 citations in OpenAlex.

  1. Article
  2. 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 at 4 institutions in 1 country.

Seungheon LeeDepartment of Pharmacological and Pharmaceutical Sciences, University of Houston, Health Building 2, Houston, TX 77204, USA.
Melissa S LoveCalibr, a Division of The Scripps Research Institute, La Jolla, CA, 92037, USA.
Ramkumar ModukuriCalibr, a Division of The Scripps Research Institute, La Jolla, CA, 92037, USA.
Arnab K ChatterjeeCalibr, a Division of The Scripps Research Institute, La Jolla, CA, 92037, USA.
Lauren HuertaCalibr, a Division of The Scripps Research Institute, La Jolla, CA, 92037, USA.
Ann P LawsonDepartment of Biology, Brandeis University, 415 South St., Waltham, MA 02454, USA.
Case W McNamaraCalibr, a Division of The Scripps Research Institute, La Jolla, CA, 92037, USA.
Jan R MeadAtlanta VA Medical Center and Department of Pediatrics, Emory University School of Medicine, Atlanta, GA 30322, USA.
Lizbeth HedstromDepartment of Biology, Brandeis University, 415 South St., Waltham, MA 02454, USA; Department of Chemistry, Brandeis University, 415 South St., Waltham, MA 02454, USA.
Gregory D CunyDepartment of Pharmacological and Pharmaceutical Sciences, University of Houston, Health Building 2, Houston, TX 77204, USA. Electronic address: gdcuny@central.uh.edu.
Scripps Research Institute · USBrandeis University · USUniversity of Houston · USEmory University · US

Funding

IMPDH inhibitors for the treatment of Cryptosporidium infectionsR01AI125362 · NIAID · UNIVERSITY OF HOUSTON · PI CUNY, GREGORY D · 2016 to 2020
$3.8M
NIAID NIH HHS R01 AI125362
6 · The paper itself

Abstract

BMS906024, a γ-secretase inhibitor that blocks Notch signaling, was previously shown to inhibit Cryptosporidium parvum growth in vitro. A structure-activity relationship (SAR) analysis of BMS906024 reported herein demonstrates the importance of the stereochemistry of the C-3 benzodiazepine and the succinyl β-substituent. However, concomitant removal of the succinyl α-substituent and switching the primary amide with secondary amides was tolerated. For example, 32 (SH287) inhibited C. parvum growth in HCT-8 host cells with an EC

Indexed as

CryptosporidiosisCryptosporidiumCryptosporidium parvumBenzodiazepinonesHumansStructure-Activity RelationshipBenzodiazepinonesBMS-906024

Identifiers

PMID37196868
PMCPMC10290938
OpenAlexW4376891765

What Socratic holds

Textmetadata
LicenceCC BY
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.