Discovery of 4-(Piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine Derivatives as Akt Inhibitors

Yang Liu; Yanzhen Yin; Jingya Zhang; Krystle Nomie; Liang Zhang; Dezhi Yang; Michael L. Wang; Guisen Zhao

doi:10.1002/ardp.201500427

Discovery of 4-(Piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine Derivatives as Akt Inhibitors

Yang Liu, Yanzhen Yin, Jingya Zhang, Krystle Nomie, Liang Zhang, Dezhi Yang, Michael L. Wang, Guisen Zhao

Lymphoma-Myeloma

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

6 Scopus citations

Abstract

A series of 4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives was synthesized and evaluated as Akt inhibitors by optimization of a weak screening lead (1). Typically, compounds 5q and 5t significantly improved the Akt1 inhibitory potency with IC ₅₀ values of 18.0 and 21.3 nM, respectively, with desirable antiproliferative effect against the cell lines LNCaP and PC-3. The inhibitors 5q and 5t might serve as lead compounds for further exploration of Akt inhibitors as anticancer agents.

Original language	English (US)
Pages (from-to)	356-362
Number of pages	7
Journal	Archiv der Pharmazie
Volume	349
Issue number	5
DOIs	https://doi.org/10.1002/ardp.201500427
State	Published - May 1 2016

Keywords

Akt
Anticancer
Docking
Pyrrolopyrimidines

ASJC Scopus subject areas

Pharmaceutical Science
Drug Discovery

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10.1002/ardp.201500427

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title = "Discovery of 4-(Piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine Derivatives as Akt Inhibitors",

abstract = " A series of 4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives was synthesized and evaluated as Akt inhibitors by optimization of a weak screening lead (1). Typically, compounds 5q and 5t significantly improved the Akt1 inhibitory potency with IC 50 values of 18.0 and 21.3 nM, respectively, with desirable antiproliferative effect against the cell lines LNCaP and PC-3. The inhibitors 5q and 5t might serve as lead compounds for further exploration of Akt inhibitors as anticancer agents.",

keywords = "Akt, Anticancer, Docking, Pyrrolopyrimidines",

author = "Yang Liu and Yanzhen Yin and Jingya Zhang and Krystle Nomie and Liang Zhang and Dezhi Yang and Wang, {Michael L.} and Guisen Zhao",

note = "Funding Information: This work was supported by the National Natural Science Foundation of China (no. 21272140) and Projects of Shandong Science and Technology (no. 2014GSF119003) Publisher Copyright: {\textcopyright} 2016 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.",

year = "2016",

month = may,

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doi = "10.1002/ardp.201500427",

language = "English (US)",

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T1 - Discovery of 4-(Piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine Derivatives as Akt Inhibitors

AU - Liu, Yang

AU - Yin, Yanzhen

AU - Zhang, Jingya

AU - Nomie, Krystle

AU - Zhang, Liang

AU - Yang, Dezhi

AU - Wang, Michael L.

AU - Zhao, Guisen

N1 - Funding Information: This work was supported by the National Natural Science Foundation of China (no. 21272140) and Projects of Shandong Science and Technology (no. 2014GSF119003) Publisher Copyright: © 2016 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.

PY - 2016/5/1

Y1 - 2016/5/1

N2 - A series of 4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives was synthesized and evaluated as Akt inhibitors by optimization of a weak screening lead (1). Typically, compounds 5q and 5t significantly improved the Akt1 inhibitory potency with IC 50 values of 18.0 and 21.3 nM, respectively, with desirable antiproliferative effect against the cell lines LNCaP and PC-3. The inhibitors 5q and 5t might serve as lead compounds for further exploration of Akt inhibitors as anticancer agents.

AB - A series of 4-(piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine derivatives was synthesized and evaluated as Akt inhibitors by optimization of a weak screening lead (1). Typically, compounds 5q and 5t significantly improved the Akt1 inhibitory potency with IC 50 values of 18.0 and 21.3 nM, respectively, with desirable antiproliferative effect against the cell lines LNCaP and PC-3. The inhibitors 5q and 5t might serve as lead compounds for further exploration of Akt inhibitors as anticancer agents.

KW - Akt

KW - Anticancer

KW - Docking

KW - Pyrrolopyrimidines

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DO - 10.1002/ardp.201500427

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Discovery of 4-(Piperazin-1-yl)-7H-pyrrolo[2,3-d]pyrimidine Derivatives as Akt Inhibitors

Abstract

Keywords

ASJC Scopus subject areas

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