Design, synthesis and activity of benzofuran-7-carboxamide poly(adp-ribose)-polymerase inhibitors

Qiu Jin; Minhang Xin; Xin Cong; Qidong You

doi:10.6023/cjoc201211019

Design, synthesis and activity of benzofuran-7-carboxamide poly(adp-ribose)-polymerase inhibitors

Qiu Jin
, Minhang Xin
, Xin Cong
, Qidong You

China Pharmaceutical University
Jiangsu Simcere Pharmaceutical Co. Ltd.

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

4 Scopus citations

Abstract

Poly-(ADP-ribose)-polymerase (PARP) is a promising anti-cancer target as it plays a crucial role in the cellular reparation and survival mechanisms. A series of benzofuran-7-carboxamides was designed to maintain the required pharmacophore conformation through an intramolecular hydrogen bond. Twelve compounds were synthesized and the inhibitory effect on PARP activity of these compounds were tested and evaluated. The results showed that all the target compounds displayed potency against the PARP enzyme, and compound 7c was the most potent one with an IC₅₀ value of 20.5 nmol·L^-1.

Original language	English
Pages (from-to)	590-595
Number of pages	6
Journal	Chinese Journal of Organic Chemistry
Volume	33
Issue number	3
DOIs	https://doi.org/10.6023/cjoc201211019
State	Published - Mar 2013
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Anti-tumor
Benzofuran-7-carboxamide
PARP inhibitor
Synthesis

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10.6023/cjoc201211019

Cite this

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title = "Design, synthesis and activity of benzofuran-7-carboxamide poly(adp-ribose)-polymerase inhibitors",

abstract = "Poly-(ADP-ribose)-polymerase (PARP) is a promising anti-cancer target as it plays a crucial role in the cellular reparation and survival mechanisms. A series of benzofuran-7-carboxamides was designed to maintain the required pharmacophore conformation through an intramolecular hydrogen bond. Twelve compounds were synthesized and the inhibitory effect on PARP activity of these compounds were tested and evaluated. The results showed that all the target compounds displayed potency against the PARP enzyme, and compound 7c was the most potent one with an IC50 value of 20.5 nmol·L-1.",

keywords = "Anti-tumor, Benzofuran-7-carboxamide, PARP inhibitor, Synthesis",

author = "Qiu Jin and Minhang Xin and Xin Cong and Qidong You",

year = "2013",

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T1 - Design, synthesis and activity of benzofuran-7-carboxamide poly(adp-ribose)-polymerase inhibitors

AU - Jin, Qiu

AU - Xin, Minhang

AU - Cong, Xin

AU - You, Qidong

PY - 2013/3

Y1 - 2013/3

N2 - Poly-(ADP-ribose)-polymerase (PARP) is a promising anti-cancer target as it plays a crucial role in the cellular reparation and survival mechanisms. A series of benzofuran-7-carboxamides was designed to maintain the required pharmacophore conformation through an intramolecular hydrogen bond. Twelve compounds were synthesized and the inhibitory effect on PARP activity of these compounds were tested and evaluated. The results showed that all the target compounds displayed potency against the PARP enzyme, and compound 7c was the most potent one with an IC50 value of 20.5 nmol·L-1.

AB - Poly-(ADP-ribose)-polymerase (PARP) is a promising anti-cancer target as it plays a crucial role in the cellular reparation and survival mechanisms. A series of benzofuran-7-carboxamides was designed to maintain the required pharmacophore conformation through an intramolecular hydrogen bond. Twelve compounds were synthesized and the inhibitory effect on PARP activity of these compounds were tested and evaluated. The results showed that all the target compounds displayed potency against the PARP enzyme, and compound 7c was the most potent one with an IC50 value of 20.5 nmol·L-1.

KW - Anti-tumor

KW - Benzofuran-7-carboxamide

KW - PARP inhibitor

KW - Synthesis

UR - https://www.scopus.com/pages/publications/84877336230

U2 - 10.6023/cjoc201211019

DO - 10.6023/cjoc201211019

M3 - 文章

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SN - 0253-2786

VL - 33

SP - 590

EP - 595

JO - Chinese Journal of Organic Chemistry

JF - Chinese Journal of Organic Chemistry

IS - 3

ER -

Design, synthesis and activity of benzofuran-7-carboxamide poly(adp-ribose)-polymerase inhibitors

Abstract

UN SDGs

Keywords

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