Suzuki coupling based synthesis and in vitro cytotoxic evaluation of Fingolimod and analogues

Tie Wen Mei; Yu Luo; Xiang Jun Feng; Wei Lu; Bo Yang

doi:10.1016/j.tet.2013.02.030

Suzuki coupling based synthesis and in vitro cytotoxic evaluation of Fingolimod and analogues

Tie Wen Mei, Yu Luo, Xiang Jun Feng, Wei Lu, Bo Yang

School of Chemistry and Molecular Engineering

Research output: Contribution to journal › Article › peer-review

9 Scopus citations

Abstract

A concise synthesis of Fingolimod (FTY720) and its analogues was described. The key step involved Suzuki coupling of arylboronate 11 with different bromides. In addition, the newly synthesized Fingolimod analogues (5a-i and 6a-c) were evaluated for their in vitro cytotoxicity against SMCC-7721 and HL-60 cell lines. The preliminary SAR was discussed.

Original language	English
Pages (from-to)	2927-2932
Number of pages	6
Journal	Tetrahedron
Volume	69
Issue number	14
DOIs	https://doi.org/10.1016/j.tet.2013.02.030
State	Published - 8 Apr 2013

Keywords

Concise synthesis
Cytotoxicity
Key step
Suzuki coupling

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10.1016/j.tet.2013.02.030

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title = "Suzuki coupling based synthesis and in vitro cytotoxic evaluation of Fingolimod and analogues",

abstract = "A concise synthesis of Fingolimod (FTY720) and its analogues was described. The key step involved Suzuki coupling of arylboronate 11 with different bromides. In addition, the newly synthesized Fingolimod analogues (5a-i and 6a-c) were evaluated for their in vitro cytotoxicity against SMCC-7721 and HL-60 cell lines. The preliminary SAR was discussed.",

keywords = "Concise synthesis, Cytotoxicity, Key step, Suzuki coupling",

author = "Mei, \{Tie Wen\} and Yu Luo and Feng, \{Xiang Jun\} and Wei Lu and Bo Yang",

year = "2013",

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volume = "69",

pages = "2927--2932",

journal = "Tetrahedron",

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T1 - Suzuki coupling based synthesis and in vitro cytotoxic evaluation of Fingolimod and analogues

AU - Mei, Tie Wen

AU - Luo, Yu

AU - Feng, Xiang Jun

AU - Lu, Wei

AU - Yang, Bo

PY - 2013/4/8

Y1 - 2013/4/8

N2 - A concise synthesis of Fingolimod (FTY720) and its analogues was described. The key step involved Suzuki coupling of arylboronate 11 with different bromides. In addition, the newly synthesized Fingolimod analogues (5a-i and 6a-c) were evaluated for their in vitro cytotoxicity against SMCC-7721 and HL-60 cell lines. The preliminary SAR was discussed.

AB - A concise synthesis of Fingolimod (FTY720) and its analogues was described. The key step involved Suzuki coupling of arylboronate 11 with different bromides. In addition, the newly synthesized Fingolimod analogues (5a-i and 6a-c) were evaluated for their in vitro cytotoxicity against SMCC-7721 and HL-60 cell lines. The preliminary SAR was discussed.

KW - Concise synthesis

KW - Cytotoxicity

KW - Key step

KW - Suzuki coupling

UR - https://www.scopus.com/pages/publications/84874665708

U2 - 10.1016/j.tet.2013.02.030

DO - 10.1016/j.tet.2013.02.030

M3 - 文章

AN - SCOPUS:84874665708

SN - 0040-4020

VL - 69

SP - 2927

EP - 2932

JO - Tetrahedron

JF - Tetrahedron

IS - 14

ER -

Suzuki coupling based synthesis and in vitro cytotoxic evaluation of Fingolimod and analogues

Abstract

Keywords

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