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Lu, Tiangong; Goh, Aik Wye; Yu, Mingfeng; Adams, Julian; Lam, Frankie; Teo, Theodosia; Li, Peng; Noll, Ben; Zhong, Longjin; Diab, Sarah; Chahrour, Osama; Hu, Anran; Abbas, Abdullahi Y,; Liu, Xiangrui; Huang, Shiliang; Sumby, Christopher J.; Milne, Robert; Midgley, Carol and Wang, Shudong
(2014).
DOI: https://doi.org/10.1021/jm4019614
Abstract
ON01910.Na is a highly effective anticancer agent that induces mitotic arrest and apoptosis. Clinical studies with ON01910 in cancer patients have shown efficacy along with an impressive safety profile. While ON01910 is highly active against cancer cells, it has a low oral availability and requires continuous intravenous infusion or multiple gram doses to ensure sufficient drug exposure for biological activity in patients. We have identified two novel series of styrylsulfonyl-methylpyridines. Lead compounds 8, 9a, 18 and 19a are highly potent mitotic inhibitors and selectively cytotoxic to cancer cells. Impressively, these compounds possess excellent pharmaceutical properties and two lead drug candidates 9a and 18 demonstrated antitumor activities in animal models.
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About
- Item ORO ID
- 40338
- Item Type
- Journal Item
- ISSN
- 1520-4804
- Academic Unit or School
-
Faculty of Science, Technology, Engineering and Mathematics (STEM) > Life, Health and Chemical Sciences
Faculty of Science, Technology, Engineering and Mathematics (STEM) - Copyright Holders
- © 2014 American Chemical Society
- Depositing User
- Carol Midgley