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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 covalent adduct formation in a sequence-selective fashion. Carzelesin… Expand
Preliminary toxicity studies with the DNA-binding antibiotic, CC-1065.
It was previously shown that the potent new DNA-binding antibiotic, CC-1065, prolonged life span, but was not curative, when administered to mice bearing a variety of transplantable tumors. In this… Expand
Adozelesin, a selected lead among cyclopropylpyrroloindole analogs of the DNA-binding antibiotic, CC-1065
- L. Li, R. C. Kelly, M. A. Warpehoski, J. P. Mcgovren, I. Gebhard, T. F. Dekoning
- Investigational New Drugs
- 1 May 1991
SummaryAdozelesin (U-73975) is a potent synthetic cyclopropylpyrroloindole (CPI) analog of the cytotoxic DNA-binding antibiotic, CC-1065. In contrast to the natural product, adozelesin and related… Expand
Isolation and identification of a major metabolite of PNU-107859, an MMP inhibitor from the biliary fluid of rats.
- M. Kuo, D. Yurek, S. A. Mizsak, Mark D. Prairie, S. Mattern, T. F. Dekoning
- Medicine, Chemistry
- Journal of pharmaceutical sciences
- 1 July 1999
PNU-107859, an important representative structure in a novel class of matrix metalloproteinases (MMP) inhibitors known as thiadiazoles, was found to be quickly eliminated from rats. A major… Expand
Preclinical antitumor activity of bizelesin in mice.
- C. A. Carter, W. R. Waud, L. Li, T. F. Dekoning, J. P. Mcgovren, J. Plowman
- Clinical cancer research : an official journal of…
- 1 July 1996
Bizelesin (U-77779, NSC 615291), a synthetic analogue of the cytotoxic antibiotic CC-1065, is a bifunctional alkylating agent that produces DNA interstrand cross-links. Bizelesin was evaluated for… Expand
Combination efficacy with MetMAb and erlotinib in a NSCLC tumor model highlight therapeutic opportunities for c-Met inhibitors in combination with EGFR inhibitors
1336 Crosstalk between EGFR and c-Met has been implicated in a number of biological systems. In tumors, interactions between these two pathways may affect tumor cell growth, survival, and response to… Expand
12,13-isotaxanes: synthesis of new potent analogs and X-ray crystallographic confirmation of structure.
Effect of mouse hepatitis virus infection on combination therapy of P388 leukemia with cyclophosphamide and pyrimidinones.
- L. Li, T. F. Dekoning, +4 authors M. J. Collins
- Biology, Medicine
- Laboratory animal science
- 1 February 1987
At least three marked differences were noted in the results compared from two parallel experiments using identical protocols with virus-free mice and mouse hepatitis virus (MHV) infected mice… Expand
Relationship between modulation of natural killer cell activity and antitumor activity of bropirimine when used in combination with various types of chemotherapeutic drugs.
Bropirimine (ABPP), a pyrimidinone, is currently under clinical trial for its antitumor potential. Bropirimine alone was marginally active against some experimental tumors such as B16 melanoma but… Expand
Antitumor activity of pyrimidinones, a class of small-molecule biological response modifiers.
- L. Li, T. Wallace, W. Wierenga, H. Skulnick, T. F. Dekoning
- Chemistry, Medicine
- Journal of biological response modifiers
- 1 February 1987
This study was undertaken in an attempt to evaluate the structure-activity relationship of pyrimidinones. Of 20 pyrimidinones tested, only those with a monohalogen substitution at the ortho- or… Expand