Analogs of sarcodictyin and eleutherobin
US5965718A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Sep 1, 1998 |
| Grant date | Oct 12, 1999 |
| Priority date | — |
| Expiry date | Sep 1, 2018 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P43/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.