发明名称 |
Analogs of sarcodictyin and eleutherobin |
摘要 |
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.
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申请公布号 |
US5965718(A) |
申请公布日期 |
1999.10.12 |
申请号 |
US19980145376 |
申请日期 |
1998.09.01 |
申请人 |
THE SCRIPPS RESEARCH INSTITUTE |
发明人 |
NICOLAOU, KYRIACOS C.;VANDELFT, FLORIS;HOSOKAWA, SEIJIRO;KIM, SANGHEE;LI, TIANHU;OHSHIMA, TAKASHI;PFEFFERKORN, JEFF;VOURLOUMIS, DIONISIOS;XU, JIN-YOU;WINSSINGER, NICOLAS |
分类号 |
C07H15/26;A61K31/34;A61K31/4164;A61K31/422;A61K31/427;A61K31/443;A61K31/7028;A61K31/7048;A61P35/00;A61P43/00;C07D493/08;C07F7/18;(IPC1-7):C07H15/24;A61K31/70;C07D307/77 |
主分类号 |
C07H15/26 |
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