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carzelesin

Known as: 2-Benzofurancarboxamide, N-(2-((1-(chloromethyl)-1,6-dihydro-8-methyl-5-(((phenylamino)carbonyl)oxy)benzo(1,2-b:4,3-b')dipyrrol-3(2H)-yl)carbonyl)-1H-indol-5-yl)-6-(diethylamino)-, (S)- 
A cyclopropylpyrroloindole prodrug analogue and DNA minor groove binding agent, with antineoplastic activity. After hydrolysis, the cyclopropyl group… 
National Institutes of Health

Related topics

Related topics

3 relations

Broader (2)

BenzofuransIndoles

Narrower (1)

U 80244

Papers overview

Semantic Scholar uses AI to extract papers important to this topic.
Review
2009
Review
2009
Chemical and biological explorations of the family of CC-1065 and the duocarmycin natural products.
CC-1065, the duocarmycins and yatakemycin are members of a family of ultrapotent antitumour antibiotics that have been the… 
Review
2000
Review
2000
Recent developments in sequence selective minor groove DNA effectors.
DNA is a well characterized intracellular target but its large size and sequential nature make it an elusive target for selective… 
2000
2000
Carzelesin phase II study in advanced breast, ovarian, colorectal, gastric, head and neck cancer, non-Hodgkin's lymphoma and malignant melanoma: a study of the EORTC early clinical studies group…
Purpose: In a phase II trial, the activity of carzelesin, a cyclopropylpyrroloindole prodrug analog, was assessed. Patients and… 
Review
1999
Review
1999
Synthetic DNA minor groove-binding drugs.
1999
1999
Comparative activity of the cyclopropylpyrroloindole compounds adozelesin, bizelesin and carzelesin in a human tumor colony-forming assay.
Adozelesin, bizelesin and carzelesin are synthetic cyclopropylpyrroloindole (CPI) analogs, a class of potent antineoplastic… 
1998
1998
A clinical pharmacokinetics study of carzelesin given by short-term intravenous infusion in a phase I study
Abstract We investigated the pharmacokinetic behavior of carzelesin in 31 patients receiving this drug by 10-min intravenous… 
1998
1998
Comparative pharmacology of the novel cyclopropylpyrroloindole-prodrug carzelesin in mice, rats, and humans.
Carzelesin is a novel cyclopropylpyrroloindole prodrug analogue that has recently been tested in Phase I clinical trials. To… 
Review
1997
Review
1997
DNA minor groove binding ligands: a new class of anticancer agents.
This paper gives an overview of the available pharmacological and clinical data of a new class of anticancer drugs which act by… 
1996
1996
Phase I clinical and pharmacokinetic study of carzelesin (U-80244) given daily for five consecutive days.
Carzelesin (U-80244), one of the synthetic DNA minor groove binding cyclopropylpyrroloindole analogues, was selected for clinical… 
Highly Cited
1992
Highly Cited
1992
Cytotoxicity and antitumor activity of carzelesin, a prodrug cyclopropylpyrroloindole analogue.
The cyclopropylpyrroloindole analogues are DNA minor-groove binders containing a cyclopropyl group, which mediates N3-adenine… 
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