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Title:
Antitumor activity of triazine mimic antibiotics for DNA-binding implications (impressive activity in vitro against a variety of tumor types in the NCI-60 screen): NSC 710607 to fight HCT-116 human colon carcinoma cell lines in vivo using the hollow fiber assay and xenograft mouse models | Journal of Cancer Research and Clinical Oncology
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Purpose Successful clinical applications of DNA-directed selective cytotoxic agents disrupt the vital replication/transcription processes and ultimately lead to cancer cell death. This study aimed to examine the growth screen of two lead triazine compounds in a number of cell lines and xenografts and to develop anticancer agents with noncovalent binding affinity bringing fewer side effects. Methods The NCI initial hollow fiber test was performed using an established procedure. The cytostatic and cytocidal capacities of the test compounds were assessed by evaluating cytotoxicity by simply performing a standard cellular viability assay. The nude mouse human tumor xenograft system was used as an in vivo model. Results More sensitive drug with sub-micromolar activity met the interdisciplinary criteria for testing and was referred to evaluations in subcutaneous colorectal carcinoma HCT-116 human tumor xenografted into nude mice. Principal findings of the study: total cytostasis, almost nontoxic schedules, specific working hypotheses, strong rationale for the potential use, and important general implications (relevance to human biology). NSC 710607 displayed in vivo better than Cisplatin and 5-fluorouracil abilities to significantly decrease tumor growth. Conclusion Cell proliferation can be reduced or stopped in vivo in view of the xenograft results. The mimic molecule behaves as DNA-binding antitumor antibiotics with great potential as general anticancer agents and deserves further trials. NSC 710607 represents the result of a design strategy with outstanding potential. This study also identifies the prognostic significance and is likely to translate to other species or systems.
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article, google, scholar, pubmed, cas, cancer, dna, anticancer, agents, spychala, human, chem, activity, synthesis, med, central, author, research, antitumor, nci, cell, binding, drug, colorectal, access, res, data, vivo, study, design, privacy, cookies, content, journal, publish, implications, tumor, hct, carcinoma, hollow, fiber, assay, xenograft, mouse, potential, httpsdoiorg, springer, information, search, clinical,
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month download article/chapter rna-specific groove-binding cations cyclic-aminotropiminium carboxylate derivatives anti-pneumocystis carinii agents covalent ligand/dna interactions hollow fiber assay dna-binding antitumor antibiotics writingโoriginal draft preparation eortc/nci worldwide activity tri-functional mononuclear platinum vital replication/transcription processes cytotoxic anticancer effects human dna topoisomerase dna binding agents full article pdf dna binding levels dna minor groove accepted manuscript version xenograft mouse models privacy choices/manage cookies cancer cell death clinical oncology aims related subjects xenografted pc3 tumors van krieken jh develop anticancer agents dna-binding implications colorectal cancer survival double stranded dna dna-topoisomerase inhibitors target dna recognition general anticancer agents crispr-cas12c1 system cell lines article spychala dna topoisomerase ii specific working hypotheses nucleic acids res jaroslaw spychala antiviral drug design anticancer efficacy studies triazine mimic antibiotics holds exclusive rights xenograft data provided micromolar activity met promising antitumor activity european economic area mimic molecule behaves molecular docking studies substituted 4-oxothiazolidin-3-yl
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headline:Antitumor activity of triazine mimic antibiotics for DNA-binding implications (impressive activity in vitro against a variety of tumor types in the NCI-60 screen): NSC 710607 to fight HCT-116 human colon carcinoma cell lines in vivo using the hollow fiber assay and xenograft mouse models
description:Successful clinical applications of DNA-directed selective cytotoxic agents disrupt the vital replication/transcription processes and ultimately lead to cancer cell death. This study aimed to examine the growth screen of two lead triazine compounds in a number of cell lines and xenografts and to develop anticancer agents with noncovalent binding affinity bringing fewer side effects. The NCI initial hollow fiber test was performed using an established procedure. The cytostatic and cytocidal capacities of the test compounds were assessed by evaluating cytotoxicity by simply performing a standard cellular viability assay. The nude mouse human tumor xenograft system was used as an in vivo model. More sensitive drug with sub-micromolar activity met the interdisciplinary criteria for testing and was referred to evaluations in subcutaneous colorectal carcinoma HCT-116 human tumor xenografted into nude mice. Principal findings of the study: total cytostasis, almost nontoxic schedules, specific working hypotheses, strong rationale for the potential use, and important general implications (relevance to human biology). NSC 710607 displayed in vivo better than Cisplatin and 5-fluorouracil abilities to significantly decrease tumor growth. Cell proliferation can be reduced or stopped in vivo in view of the xenograft results. The mimic molecule behaves as DNA-binding antitumor antibiotics with great potential as general anticancer agents and deserves further trials. NSC 710607 represents the result of a design strategy with outstanding potential. This study also identifies the prognostic significance and is likely to translate to other species or systems.
datePublished:2023-02-13T00:00:00Z
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HCT-116 colorectal carcinoma
Hollow fiber assay
Large-scale NCI-60
Mechanisms of cancer
Mouse xenografts
MV-3 human melanoma
Oncology
Cancer Research
Internal Medicine
Hematology
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headline:Antitumor activity of triazine mimic antibiotics for DNA-binding implications (impressive activity in vitro against a variety of tumor types in the NCI-60 screen): NSC 710607 to fight HCT-116 human colon carcinoma cell lines in vivo using the hollow fiber assay and xenograft mouse models
description:Successful clinical applications of DNA-directed selective cytotoxic agents disrupt the vital replication/transcription processes and ultimately lead to cancer cell death. This study aimed to examine the growth screen of two lead triazine compounds in a number of cell lines and xenografts and to develop anticancer agents with noncovalent binding affinity bringing fewer side effects. The NCI initial hollow fiber test was performed using an established procedure. The cytostatic and cytocidal capacities of the test compounds were assessed by evaluating cytotoxicity by simply performing a standard cellular viability assay. The nude mouse human tumor xenograft system was used as an in vivo model. More sensitive drug with sub-micromolar activity met the interdisciplinary criteria for testing and was referred to evaluations in subcutaneous colorectal carcinoma HCT-116 human tumor xenografted into nude mice. Principal findings of the study: total cytostasis, almost nontoxic schedules, specific working hypotheses, strong rationale for the potential use, and important general implications (relevance to human biology). NSC 710607 displayed in vivo better than Cisplatin and 5-fluorouracil abilities to significantly decrease tumor growth. Cell proliferation can be reduced or stopped in vivo in view of the xenograft results. The mimic molecule behaves as DNA-binding antitumor antibiotics with great potential as general anticancer agents and deserves further trials. NSC 710607 represents the result of a design strategy with outstanding potential. This study also identifies the prognostic significance and is likely to translate to other species or systems.
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HCT-116 colorectal carcinoma
Hollow fiber assay
Large-scale NCI-60
Mechanisms of cancer
Mouse xenografts
MV-3 human melanoma
Oncology
Cancer Research
Internal Medicine
Hematology
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