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anthracene derivative/cáncer
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A novel anthracene derivative, MHY412, induces apoptosis in doxorubicin-resistant MCF-7/Adr human breast cancer cells through cell cycle arrest and downregulation of P-glycoprotein expression.
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New potential chemotherapeutic strategies are required to overcome multidrug resistance (MDR) in cancer. This study investigated the anticancer effect of a novel anthracene derivative MHY412 on doxorubicin-resistant human breast cancer (MCF-7/Adr) cells. We measured cell viability and the expression
Anti-tumour effects of HL-37, a novel anthracene derivative, in-vivo and in-vitro.
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Many anthracene derivatives possess excellent anti-tumour activity and are extensively used clinically as anti-tumour agents. However, their clinical use is frequently limited by emergence of multidrug resistance (MDR) in tumour cells. Therefore, new agents with the ability to overcome MDR are
HL-37, a novel anthracene derivative, induces Ca(2+)-mediated apoptosis in human breast cancer cells.
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HL-37, a novel anthracene derivative, exhibited potent anticancer activity in many kinds of cancer cells. However, the exact mechanism and signaling pathway involved in HL-37-induced apoptosis have not been fully elucidated. Therefore, we explored the mechanisms of HL-37-mediated apoptosis in MCF-7
Synthesis, cytotoxicity and DNA binding of oxoazabenzo[de]anthracenes derivatives in colon cancer Caco-2 cells.
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New oxoazabenzo[de]anthracenes derivatives were synthesised and characterised. Their interactions with calf thymus DNA were studied by UV spectrophotometric analysis and a competitive ethidium bromide displacement assay. Cytotoxicity was determined by MTT assay, against colon adenocarcinoma (Caco-2
Phase I clinical and pharmacokinetic study of bisantrene in refractory pediatric solid tumors.
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Fourteen patients with pediatric malignant solid tumors, median age 15 years, received 22 courses of bisantrene in a Phase I study. Dosage escalations ranged from 10 to 120 mg/m2 daily for 5 consecutive days. Toxicity included myelosuppression and phlebitis. A sensitive (detection limit of 2 ng/ml)
Activity of 9-10 anthracenedicarboxaldehyde bis[(4,5-dihydro-1 H-imidazol-2-yl)hydrazone]dihydrochloride (CL216,942) in a human tumor cloning system. Leads for phase II trials in man.
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We have utilized a recently developed human tumor cloning system to screen for antitumor effects in vitro of a new anthracene derivative, CL216,942. The object was to determine whether the system is useful for pinpointing the types of tumors in patients which should be studied in early phase II
Comparison of cytotoxicity in heart cells and tumor cells exposed to DNA intercalating agents in vitro.
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A new approach to antitumor analog selection was evaluated using in vitro cytotoxicity assays in tumor cells and heart cells. Eight anthracycline antibiotics and five non-anthracycline DNA intercalating agents were separately exposed to human 8226 myeloma cells and neonatal rat heart myocytes in
A phase I trial of vinorelbine in combination with mitoxantrone in patients with refractory solid tumors.
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Vinorelbine (Navelbine) is a unique semi-synthetic vinca-alkaloid with a favorable safety profile that has demonstrated significant antitumor activity in patients with non-small cell lung cancer, advanced breast cancer, advanced ovarian cancer and Hodgkin's disease. The most common dose-limiting
Potential and problems with growth of breast cancer in a human tumor cloning system.
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A human tumor cloning system has been utilized to culture 431 patients' breast cancer specimens. Overall, 288 or 67% of the specimens formed colonies in soft agar. Of the primary lesions 188/260 (72%) formed colonies and 100/171 (58%) of the metastatic lesions formed colonies. The median number of
A randomized trial of doxorubicin, mitoxantrone and bisantrene in advanced breast cancer (a South West Oncology Group Study).
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New agents with increased activity and/or reduced toxicity are needed for the treatment of advanced breast cancer. The anthracene derivatives mitoxantrone and bisantrene had significant activity and acceptable toxicity in phase II trials. In an ongoing phase III trial we have now randomized 150
Selective photocytotoxicity of anthrols on cancer stem-like cells: The effect of quinone methides or reactive oxygen species.
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Cancer stem cells (CSCs) are a subpopulation of cancer cells that share properties of embryonic stem cells like pluripotency and self-renewal and show increased resistance to chemo- and radiotherapy. Targeting CSC, rather than cancer cells in general, is a novel and promising strategy for cancer
Cellular accumulation and DNA platination of two new platinum(II) anticancer compounds based on anthracene derivatives as carrier ligands.
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The anticancer properties of two new fluorescent platinum(II) compounds, cis-[Pt(A9opy)Cl(2)] and cis-[Pt(A9pyp)(dmso)Cl(2)] are described. These compounds are highly active against several human tumor cell lines, including human ovarian carcinoma sensitive and cisplatin-resistant cell lines (A2780
Carcinogenic activity of some benz(a)anthracene derivatives in newborn mice.
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Equimolar doses of 7-methylbenz(a)anthracene and 3 of its derivatives were given to newborn male and female Swiss mice. All 4 substances tested increased the risk of tumour development compared with that seen in control mice given the vehicle, arachis oil, only.7-Methylbenz(a)anthracene itself was
Targeting Canine KIT Promoter by Candidate DNA G-Quadruplex Ligands.
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G-quadruplexes (G4) are nucleic acid secondary structures frequently assumed by G-rich sequences located mostly at telomeres and proto-oncogenes promoters. Recently, we identified, in canine KIT (v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog) promoter, two G-rich sequences able to
Phase II evaluation of bisantrene in patients with advanced non-small cell lung carcinoma.
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Fourteen patients with measurable non-small cell lung cancer, who had not received prior chemotherapy, were treated with the anthracene derivative bisantrene. Although treatment was well tolerated, no antitumor activity was observed and all but two patients demonstrated disease progression before
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