The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Oct. 12, 1999
Filed:
Sep. 01, 1998
Kyriacos C Nicolaou, La Jolla, CA (US);
Floris VanDelft, Leiden, NL;
Seijiro Hosokawa, Tokyo, JP;
Sanghee Kim, Waukegan, IL (US);
Tianhu Li, San Diego, CA (US);
Takashi Ohshima, San Diego, CA (US);
Jeff Pfefferkorn, San Diego, CA (US);
Dionisios Vourloumis, San Diego, CA (US);
Jin-You Xu, La Jolla, CA (US);
Nicolas Winssinger, La Jolla, CA (US);
The Scripps Research Institute, La Jolla, CA (US);
Abstract
Sarcodictyin A and B, eleutherobin, and bioactive analogs thereof synthesized using solid phase and solution phase chemistries. The synthetic method employs an attachment of common precursors, e.g., compounds 1880 or 200, on a solid support for generating conjugates 230 and 240, followed by standard chemical manipulations. A combinatorial library of sarcodictyins and eletherobin analogs was constructed with modified C-8 ester, C-15 ester and C-4 ketal functionalities and was screened for activity with respect to tubulin polymerization and cytotoxic activity against tumor cells, including Taxol-resistant lines. Compounds 600, 610, 630, 660-700, 730, 760, 850, and 920 were identified to be of equal or superior biological activities as compared to their corresponding natural product.