Negishi cross-coupling reaction as a route to isocombretastatins

Yulia B. Malysheva, Svetlana Y. Buchvalova, Elena V. Svirshchevskaya, Valery V. Fokin, Alexey Y. Fedorov

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

Abstract

A series of isocombretastatins A has been synthesized by a new method based on the Negishi cross-coupling reaction in 19-84% yields. Five of the synthesized compounds exhibit high cytotoxic activity in nanomolar concentrations (IC₅₀ = 1-100 n) towards Jurkat, K562, Colo357, and A549 cell lines.

Original language	English
Article number	ST-2013-B0387-L
Pages (from-to)	1772-1776
Number of pages	5
Journal	Synlett
Volume	24
Issue number	14
DOIs	https://doi.org/10.1055/s-0033-1339334
Publication status	Published - 2013
Externally published	Yes

Keywords

antitubulin agents
cytotoxicity
isocombretastatins
Negishi cross-coupling
turbo Grignard reagent

ASJC Scopus subject areas

Organic Chemistry

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10.1055/s-0033-1339334

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title = "Negishi cross-coupling reaction as a route to isocombretastatins",

abstract = "A series of isocombretastatins A has been synthesized by a new method based on the Negishi cross-coupling reaction in 19-84% yields. Five of the synthesized compounds exhibit high cytotoxic activity in nanomolar concentrations (IC50 = 1-100 n) towards Jurkat, K562, Colo357, and A549 cell lines.",

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T1 - Negishi cross-coupling reaction as a route to isocombretastatins

AU - Malysheva, Yulia B.

AU - Buchvalova, Svetlana Y.

AU - Svirshchevskaya, Elena V.

AU - Fokin, Valery V.

AU - Fedorov, Alexey Y.

PY - 2013

Y1 - 2013

N2 - A series of isocombretastatins A has been synthesized by a new method based on the Negishi cross-coupling reaction in 19-84% yields. Five of the synthesized compounds exhibit high cytotoxic activity in nanomolar concentrations (IC50 = 1-100 n) towards Jurkat, K562, Colo357, and A549 cell lines.

AB - A series of isocombretastatins A has been synthesized by a new method based on the Negishi cross-coupling reaction in 19-84% yields. Five of the synthesized compounds exhibit high cytotoxic activity in nanomolar concentrations (IC50 = 1-100 n) towards Jurkat, K562, Colo357, and A549 cell lines.

KW - antitubulin agents

KW - cytotoxicity

KW - isocombretastatins

KW - Negishi cross-coupling

KW - turbo Grignard reagent

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