Abstract
We herein report the synthesis and antitumor activity of E7070 analogues containing a 3-pyridinesulfonamide moiety. E7070 was selected from our sulfonamide-based compound collections, currently undergoing Phase II clinical trials because of its tolerable toxicity profile and some antitumor responses in the Phase I setting. Of the analogues examined, ER-35745, a 6-amino-3-pyridinesulfonamide derivative, demonstrated significant oral efficacy against the HCT116 human colon carcinoma xenograft in nude mice.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Antineoplastic Agents / therapeutic use
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Carcinoma / drug therapy
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Carcinoma / pathology
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Colon / pathology
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Colonic Neoplasms / drug therapy
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Colonic Neoplasms / pathology
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Humans
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Mice
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Mice, Nude
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Molecular Structure
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis*
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Sulfonamides / chemistry
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Sulfonamides / pharmacology*
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Sulfonamides / therapeutic use
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Tumor Cells, Cultured
Substances
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Antineoplastic Agents
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Sulfonamides