E7070, a novel sulphonamide agent with potent antitumour activity in vitro and in vivo |
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| Affiliation: | 1. Brain Korea 21 PLUS Project for Medical Science, Yonsei University, Seoul, Korea;2. Department of Laboratory Medicine, Yonsei University College of Medicine, Seoul, Korea;3. Division of Hematology, Department of Internal Medicine, Yonsei University College of Medicine, Seoul, Korea;4. Department of Laboratory Medicine, Yonsei University College of Medicine, Seoul, Korea;5. Department of Laboratory Medicine, Yonsei University College of Medicine, Seoul, Korea;1. Department of Genetics and Genomic Sciences, Institute for Next Generation Healthcare and Icahn School of Medicine at Mount Sinai, New York, NY, USA;1. Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow 226 031, India;2. Division of Parasitology, CSIR-Central Drug Research Institute, Lucknow 226 031, India;3. Department of Chemistry, University of Lucknow, Lucknow 226 001, India;1. Department of Internal Medicine, Seoul National University Hospital, Seoul, South Korea;2. Department of Internal Medicine, Kyungpook National University Hospital, Daegu, South Korea;3. National Evidence-Based Healthcare Collaborating Agency, Seoul, South Korea;4. Department of Internal Medicine, Samsung Medical Center, Seoul, South Korea;5. Hematologic Oncology Clinic, Center for Specific Organs Cancer, National Cancer Center, Goyang, South Korea;6. Cancer Research Institute, Seoul National University College of Medicine, Seoul, South Korea;7. Biomedical Research Institute, Seoul National University Hospital, Seoul, South Korea;1. Department of Medical Oncology, Hospital Clínico Universitario, INCLIVA Biomedical Research Institute, University of Valencia, Valencia, Spain;2. CIBERONC, Instituto de Salud Carlos III, Madrid, Spain;3. Department of Pathology, Hospital Clínico Universitario, INCLIVA Biomedical Research Institute, University of Valencia, Valencia, Spain;1. Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, CA 92121, USA;2. Cardiovascular Institute and Department of Medicine, Stanford University, 300 Pasteur Dr., MC-5501, Stanford, CA 94305, USA |
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| Abstract: | E7070 (N-(3-Chloro-7-indolyl)-1,4-benzenedisulphonamide) was selected from our sulphonamide compound collections via antitumour screening and flow cytometric analysis. Following treatment with E7070, the cell cycle progression of P388 murine leukaemia cells was disturbed in the G1 phase. The cell-killing effect on human colon cancer HCT116 cells was found to be time-dependent. In the panel of 42 human tumour cell lines, E7070 showed an antitumour spectrum that was distinct from those of other anticancer drugs used in clinic. Animal tests using human tumour xenograft models demonstrated that E7070 could cause not only tumour growth suppression, but also tumour regression in three of five colorectal and two of two lung cancers. In the HCT116 xenograft model, E7070 was shown to be superior to 5-FU, MMC and CPT-11 (irinotecan). Furthermore, complete regression of advanced LX-1 tumours was observed in 80% of E7070-treated mice. All of these observations have promoted this drug to clinical evaluation. |
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