Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Experiment Videos

Structure-activity studies on 2-aryl-4H-3,1-benzoxazin-4-ones

J A Hadfield1, V H Pavlidis, A T McGown

  • 1CRC Department of Experimental Chemotherapy, Paterson Institute for Cancer Research, Christie Hospital, Manchester, UK.

Anti-Cancer Drugs
|October 1, 1994
PubMed
Summary
This summary is machine-generated.

Related Concept Videos

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

An 11-year retrospective review of venlafaxine ingestion in children from the California Poison Control System.

Human & experimental toxicology·2015
Same author

The impact of brief tobacco treatment training on practice behaviours, self-efficacy and attitudes among healthcare providers.

International journal of clinical practice·2014
Same author

Anti-TNF-α therapy for renal amyloid as a complication of Crohn's disease.

QJM : monthly journal of the Association of Physicians·2013
Same author

The Nature and Cause of Phobias, with Special Reference to Syphilophobia.

The British journal of venereal diseases·2011
Same author

Comparative action of methyl and isopropyl methane sulphonates on the peripheral leucocyte count in monkeys.

Nature·2010
Same author

War Neurosis: A Year in a Neuropathic Hospital-I.

British medical journal·2010
Same journal

Akt inhibitor-IV in estrogen receptor-positive breast cancer cells: cytotoxic, apoptotic, transcriptional, and in-silico comparison with tamoxifen.

Anti-cancer drugs·2026
Same journal

Prolonged multimodal disease control with trifluridine/tipiracil plus bevacizumab in KRAS-mutant metastatic rectal cancer: a case report.

Anti-cancer drugs·2026
Same journal

Growth differentiation factor-11 inhibits the progression of acute myeloid leukemia and increases chemosensitivity by inhibiting cathepsin S.

Anti-cancer drugs·2026
Same journal

Inavolisib and lenvatinib for PIK3CA-mutated refractory splenic angiosarcoma: a case report.

Anti-cancer drugs·2026
Same journal

Drug repurposing of liver cancer based on multimodal neural network and virtual screening.

Anti-cancer drugs·2026
Same journal

Discovery of an orally active and liver-targeted dual prodrug of 5-fluoro-2'-deoxyuridine-5'-monophosphate for the treatment of hepatocellular carcinoma.

Anti-cancer drugs·2026
See all related articles

Two novel benzoxazin-4-ones demonstrate significant cytotoxicity against P388 cancer cells. One compound also impacts cell cycle distribution and inhibits porcine pancreatic elastase, suggesting potential therapeutic applications.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Cancer Research

Background:

  • Benzoxazin-4-ones are a class of heterocyclic compounds with diverse biological activities.
  • Previous research has explored their potential in various therapeutic areas.
  • Structure-activity relationships are crucial for optimizing drug candidates.

Purpose of the Study:

  • To synthesize and evaluate the cytotoxicity of novel benzoxazin-4-one derivatives.
  • To identify compounds with potent anti-cancer activity in relevant cell systems.
  • To investigate the mechanism of action and structure-activity relationships of active compounds.

Main Methods:

  • Synthesis of eight benzoxazin-4-one analogs.
  • Cytotoxicity assays performed in two distinct cell systems, including P388 cells.

Related Experiment Videos

  • Cell cycle distribution analysis and enzyme inhibition assays (porcine pancreatic elastase).

    • Main Results:

    • Two benzoxazin-4-ones (compounds 3 and 10) exhibited significant cytotoxicity against P388 cells with IC50 values of 9.9 and 8.9 microM, respectively.
    • Nitrobenzoxazin-4-one (compound 10) demonstrated a notable effect on P388 cell cycle distribution.
    • Compound 10 also proved to be an inhibitor of porcine pancreatic elastase.

    Conclusions:

    • Benzoxazin-4-one derivatives show promise as cytotoxic agents against cancer cells.
    • Compound 10 displays a dual mechanism of action, affecting cell cycle and enzyme activity.
    • Further investigation into structure-activity relationships can guide the development of more potent therapeutic agents.