A new antitumor substance, BE-13793C, produced by a streptomycete. Taxonomy, fermentation, isolation, structure determination and biological activity.

Kojiri, Katsuhisa; Kondo, Hisao; Yoshinari, Tomoko; Arakawa, Hiroharu; Nakajima, Shigeru; Satoh, Fumio; Kawamura, Kenji; Okura, Akira; Suda, Hiroyuki; Okanishi, Masanori

doi:10.7164/antibiotics.44.723

Cited by 52 publications

(31 citation statements)

References 16 publications

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“…We previously developed the anti-tumor agents BE-13793C, 8) ED-110 9,10) and NB-506. 1, 2) NB-506 is an indolocarbazole compound targeting topoisomerase I.…”

Section: Discussionmentioning

confidence: 99%

In vivo Anti‐tumor Activity of a Novel Indolocarbazole Compound, J‐107088, on Murine and Human Tumors Transplanted into Mice

Arakawa¹,

Morita²,

Kodera³

et al. 1999

Japanese Journal of Cancer Research

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The ratio of LD 10 /GID 75 indicates the therapeutic window of an anti-tumor agent. Although the ratios of doxorubicin, paclitaxel and cisplatin against PC-3 were < < < <0.3, < < < <0.5 and < < < <0.2, J-107088 showed the widest therapeutic window among the anti-tumor drugs tested. J-107088 was also effective on cells that had acquired resistance related to P-glycoprotein. Furthermore, J-107088 was found to be highly effective in inhibiting proliferation of micro-metastases of tumors to the liver in mice. Therefore, J-107088 is considered to be a promising candidate as an anti-tumor drug for treatment of solid tumors in humans.

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“…We previously developed the anti-tumor agents BE-13793C, 8) ED-110 9,10) and NB-506. 1, 2) NB-506 is an indolocarbazole compound targeting topoisomerase I.…”

Section: Discussionmentioning

confidence: 99%

In vivo Anti‐tumor Activity of a Novel Indolocarbazole Compound, J‐107088, on Murine and Human Tumors Transplanted into Mice

Arakawa¹,

Morita²,

Kodera³

et al. 1999

Japanese Journal of Cancer Research

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“…[10] BE-13793C is an indolocarbazole, an indole fused to a carbazole (Figure 2), which is a moiety that appears commonly in topoisomerase inhibitors. [11] Although initially BE-13793C wasn't tested on any brain tumour cell lines, it was shown to inhibit the growth of certain leukemia cell lines, and was used as a lead compound for subsequently developed compounds, which ultimately were active against various brain tumour cell lines.…”

Section: Topoisomerase Inhibitorsmentioning

confidence: 99%

Heterocyclic scaffolds as promising anticancer agents against tumours of the central nervous system: Exploring the scope of indole and carbazole derivatives

Sherer

Snape

2015

European Journal of Medicinal Chemistry

133

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HIGHLIGHTS• Brain cancer mortality rates are much higher than mortality rates for cancers of other sites. •Due to the blood brain barrier, many drugs that work on cancers of other sites do not work on brain cancers • Indoles, carbazoles and indolocarbazoles make good scaffolds for drugs to be built up around due to their rigidity, planarity and ease of synthesis. GRAPHICAL ABSTRACT ACRONYMS/INITIALISMSAML -Acute myeloid leukaemia CK2 -Casein kinase 2 CNS -Central nervous system PARP -Poly ADP ribose polymerase PDGF -Platelet-derived growth factor PKC -Protein kinase C ROS -Reactive oxygen species VEGF -Vascular endothelial growth factor ABSTRACT Tumours of the central nervous system are intrinsically more dangerous than tumours at other sites, and in particular, brain tumours are responsible for 3% of cancer deaths in the UK. Despite this, research into new therapies only receives 1% of national cancer research spend. The most common chemotherapies are temozolomide, procarbazine, carmustine, lomustine and vincristine, but because of the rapid development of chemoresistance, these drugs alone simply aren't sufficient for longterm treatment. Such poor prognosis of brain tumour patients prompted us to research new treatments for malignant glioma, and in doing so, it became apparent that aromatic heterocycles play an important part, especially the indole, carbazole and indolocarbazole scaffolds. This review highlights compounds in development for the treatment of tumours of the central nervous system which are structurally based on the indole, carbazole and indolocarbazole scaffolds, under the expectation that it will highlight new avenues for research for the development of new compounds to treat these devastating neoplasms.

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“…staurosporeus AM-2282, K252a from Nocardiopsis sp. K252 4) , and BE-13793C from Streptoverticillium mobaraense BA13793 5) . Although the chemical structures of the indolocarbazole compounds have been noted for many years, little is known about the molecular machinery required for the formation of the indolocarbazole skeleton.…”

Section: Introductionmentioning

confidence: 99%

Biosynthesis of Heterocyclic Antibiotics in Actinomycetes and an Approach to Synthesize the Natural Compounds

Onaka

2006

Actinomycetologica

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A new antitumor substance, BE-13793C, produced by a streptomycete. Taxonomy, fermentation, isolation, structure determination and biological activity.

Cited by 52 publications

References 16 publications

In vivo Anti‐tumor Activity of a Novel Indolocarbazole Compound, J‐107088, on Murine and Human Tumors Transplanted into Mice

In vivo Anti‐tumor Activity of a Novel Indolocarbazole Compound, J‐107088, on Murine and Human Tumors Transplanted into Mice

Heterocyclic scaffolds as promising anticancer agents against tumours of the central nervous system: Exploring the scope of indole and carbazole derivatives

Biosynthesis of Heterocyclic Antibiotics in Actinomycetes and an Approach to Synthesize the Natural Compounds

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