Analogs of sarcodictyin and eleutherobin

Details Analogs of sarcodictyin and eleutherobin Analogs of sarcodictyin and eleutherobin

1998-09-01

1999-10-12

Lee, Howard C.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

514 28, 514 63, 514277, 514365, 514374, 514385, 514396, 514406, 514461, 514469, 514691, 514703, 536 174, 548146, 548215, 5483001, 549456, 549462, 549463, C07H 1524, A61K 3170, A61K 3134, C07D30777

Patent

active

059657189

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.

REFERENCES:
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