Synthesis and biological evaluation of a conformationally free seco-analogue of the immunosuppressant FR901483

被引：26

作者：

Bonjoch, J ^{[1
]}

Diaba, F

Puigbó, G

Solé, D

Segarra, V

Santamaría, L

Beleta, J

Ryder, H

Palacios, JM

机构：

[1] Univ Barcelona, Fac Pharm, Organ Chem Lab, E-08028 Barcelona, Spain

[2] Almirall Prodesfarma, Res Ctr, Barcelona 08024, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1999年 / 7卷 / 12期

关键词：

immunological activity; natural products; phosphonic acid and derivatives; poliycyclic heterocyclic compounds;

D O I：

10.1016/S0968-0896(99)00250-3

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The synthesis of an azaspirocyclic analogue of FR901483, phosphate 2, is described based on the implementation of a key 5-endo aminocyclization promoted by iodine for direct functionalization of the 1-azaspiro[4.5]decane ring at the C-3 atom. Compound 2 has no inhibitory activity in the cell proliferation assays reported. (C) 1999 Elsevier Science Ltd. All rights reserved.

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收藏

页码：2891 / 2897

页数：7

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