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.
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Authors | Takashi Owa, Hiroshi Yoshino, Tatsuo Okauchi, Tadashi Okabe, Yoichi Ozawa, Naoko Hata Sugi, Kentaro Yoshimatsu, Takeshi Nagasu, Nozomu Koyanagi, Kyosuke Kitoh |
Journal | Bioorganic & medicinal chemistry letters
(Bioorg Med Chem Lett)
Vol. 12
Issue 16
Pg. 2097-100
(Aug 19 2002)
ISSN: 0960-894X [Print] England |
PMID | 12127512
(Publication Type: Journal Article)
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Chemical References |
- Antineoplastic Agents
- Sulfonamides
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Topics |
- Animals
- Antineoplastic Agents
(chemical synthesis, chemistry, pharmacology, therapeutic use)
- Carcinoma
(drug therapy, pathology)
- Colon
(pathology)
- Colonic Neoplasms
(drug therapy, pathology)
- Humans
- Mice
- Mice, Nude
- Molecular Structure
- Structure-Activity Relationship
- Sulfonamides
(chemical synthesis, chemistry, pharmacology, therapeutic use)
- Tumor Cells, Cultured
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