Results 211 to 220 of about 32,790 (255)

Preclinical and phase I trials of topoisomerase I inhibitors

Cancer Chemotherapy and Pharmacology, 1994
A total of three topoisomerase I inhibitors, including topotecan, CPT-11 (irinotecan), and intoplicine, have been studied in both preclinical and clinical/clinical pharmacology studies. In in vitro testing against human tumor colony-forming units, all three compounds were significantly more effective when tested as a continuous exposure as compared ...
D D, Von Hoff, H A, Burris, J, Eckardt, M, Rothenberg, S M, Fields, S F, Chen, J G, Kuhn   +6 more
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β-Carbolinedione Derivatives as Topoisomerase I Inhibitors

Archiv der Pharmazie, 1999
Pyrrolo[3,4-c]-beta-carbolinedione dimers 5-14 were synthesized from furo[3,4-c]-beta-carbolinediones and diamines by solvent-free TaCl5/silica catalyzed reaction under microwave irradiation. The inhibitory property of these target compounds, the starting materials 2, 31, 32, and the N-alkylated pyrrolo[3,4-c]-beta-carbolinediones 16, 17, 20-30 was ...
S, Mahboobi, S, Eluwa, S, Kumar, M, Koller, K, Störl   +4 more
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A Series of Enediynes as Novel Inhibitors of Topoisomerase I

Bioorganic & Medicinal Chemistry, 2001
A series of acyclic enediynes, 2-((6-substituted)-3-hexen-1,5-diynyl)benzonitriles (8--11), display potent inhibition against topoisomerase I without the formation of active biradical intermediates and show inhibitory activity against topoisomerase I at 10 microM, which is five times that of camptothecin from the results of agarose gel electrophoresis.
C F, Lin, P C, Hsieh, W D, Lu, H F, Chiu, M J, Wu   +4 more
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Diversity of DNA topoisomerases I and inhibitors

Biochimie, 1998
The present review first describes the different type I topoisomerases found in eukaryotic cells: nuclear topoisomerase I (top1), topoisomerase 3 (top3), mitochondrial topoisomerase I and viral topoisomerases I. The second part of the review provides extensive information on the topoisomerase I inhibitors identified to date.
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3-Arylisoquinolines as novel topoisomerase I inhibitors

Bioorganic & Medicinal Chemistry, 2011
Topoisomerase I (topo I) is an essential enzyme for vital cellular processes. Inhibition of topo I activities is lethal and leads to cell death, thus establishing topo I as a promising target for cancer treatment. Camptothecin, a natural alkaloid, inhibits topo I.
Daulat Bikram, Khadka, Won-Jea, Cho
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Topoisomerase I Inhibitors: An Overview of the Camptothecin Analogs

Hematology/Oncology Clinics of North America, 1994
The topoisomerase I inhibitors are an exciting new class of antineoplastic agents currently under clinical development. Analogues of camptothecin with improved toxicity profiles and antitumor activity included CPT-11 and topotecan. CPT-11 has demonstrated activity against a variety of tumor types, particularly colon and lung cancer.
H A, Burris, S M, Fields
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Natural Inhibitors of DNA Topoisomerase I with Cytotoxicities

Chemistry & Biodiversity, 2008
AbstractDNA Topoisomerase I can cause DNA breaks and play a key role during cell proliferation and differentiation. It is an important target for anticancer agents. While screening for anticancer compounds, seven natural compounds, 1–7, showed potent cytotoxicities against a panel of ten cancer cell lines.
Hong-Jin, Han, Ning-Hua, Tan, Guang-Zhi, Zeng, Jun-Ting, Fan, Huo-Qiang, Huang, Chang-Jiu, Ji, Rui-Rui, Jia, Qin-Shi, Zhao, Ying-Jun, Zhang, Xiao-Jiang, Hao, Li-Qin, Wang   +10 more
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Topoisomerase I Inhibitors – The Camptothecins

2010
The camptothecins are a class of antineoplastic agents that inhibit the enzyme DNA topoisomerase I and have established activity in the treatment of various human malignancies. Camptothecin (CPT) was originally isolated in 1966 from the bark and stem of the native Chinese tree, Campotheca acuminate [155].
Michael Newton, Gene Wetzstein, Daniel Sullivan   +2 more
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Topoisomerase I inhibitors: selectivity and cellular resistance

Drug Resistance Updates, 1999
Topoisomerase I (top1) inhibitors (camptothecins and other structurally diverse compounds) are effective and promising anticancer agents. Determinants of selectivity toward cancer cells and resistance are multifactorial. These factors can be separated in three groups. The first is related to alterations in drug distribution and metabolism.
Pommier, Yves, Pourquier, Philippe, Urasaki, Yoshimasa, Wu, Jiaxi, Laco, Gary   +4 more
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Novel camptothecin derivatives as topoisomerase I inhibitors

Expert Opinion on Therapeutic Patents, 2009
Camptothecin (CPT), a pentacyclic alkaloid isolated by Wall et al. in 1958 from the Chinese tree Camptotheca acuminata, was reported to possess an interesting antitumor activity. Late in 1985, it was reported by Liu et al. that the cytotoxic activity of CPT was attributed to a novel mechanism of action involving the nuclear enzyme classified as type I ...
BASILI, SERENA, MORO, STEFANO
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