Scaffold repurposing of old drugs towards new cancer drug discovery

Haijun Chen, Jianlei Wu, Yu Gao, Haiying Chen, Jia Zhou

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

As commented by the Nobelist James Black that “The most fruitful basis of the discovery of a new drug is to start with an old drug”, drug repurposing represents an attractive drug discovery strategy. Despite the success of several repurposed drugs on the market, the ultimate therapeutic potential of a large number of non-cancer drugs is hindered during their repositioning due to various issues including the limited efficacy and intellectual property. With the increasing knowledge about the pharmacological properties and newly identified targets, the scaffolds of the old drugs emerge as a great treasure-trove towards new cancer drug discovery. In this review, we summarize the recent advances in the development of novel small molecules for cancer therapy by scaffold repurposing with highlighted examples. The relevant strategies, advantages, challenges and future research directions associated with this approach are also discussed.

Original languageEnglish (US)
Pages (from-to)2107-2114
Number of pages8
JournalCurrent Topics in Medicinal Chemistry
Volume16
Issue number19
StatePublished - Aug 1 2016

Fingerprint

Drug Repositioning
Drug Discovery
Pharmaceutical Preparations
Neoplasms
Intellectual Property
Pharmacology
Therapeutics

Keywords

  • Cancer therapeutics
  • Drug discovery
  • Drug repurposing
  • Scaffold repurposing
  • Structure-activity relationships (SARs)

ASJC Scopus subject areas

  • Drug Discovery

Cite this

Scaffold repurposing of old drugs towards new cancer drug discovery. / Chen, Haijun; Wu, Jianlei; Gao, Yu; Chen, Haiying; Zhou, Jia.

In: Current Topics in Medicinal Chemistry, Vol. 16, No. 19, 01.08.2016, p. 2107-2114.

Research output: Contribution to journalArticle

Chen, Haijun ; Wu, Jianlei ; Gao, Yu ; Chen, Haiying ; Zhou, Jia. / Scaffold repurposing of old drugs towards new cancer drug discovery. In: Current Topics in Medicinal Chemistry. 2016 ; Vol. 16, No. 19. pp. 2107-2114.
@article{203e13a7cc034597a12d57635eee3f25,
title = "Scaffold repurposing of old drugs towards new cancer drug discovery",
abstract = "As commented by the Nobelist James Black that “The most fruitful basis of the discovery of a new drug is to start with an old drug”, drug repurposing represents an attractive drug discovery strategy. Despite the success of several repurposed drugs on the market, the ultimate therapeutic potential of a large number of non-cancer drugs is hindered during their repositioning due to various issues including the limited efficacy and intellectual property. With the increasing knowledge about the pharmacological properties and newly identified targets, the scaffolds of the old drugs emerge as a great treasure-trove towards new cancer drug discovery. In this review, we summarize the recent advances in the development of novel small molecules for cancer therapy by scaffold repurposing with highlighted examples. The relevant strategies, advantages, challenges and future research directions associated with this approach are also discussed.",
keywords = "Cancer therapeutics, Drug discovery, Drug repurposing, Scaffold repurposing, Structure-activity relationships (SARs)",
author = "Haijun Chen and Jianlei Wu and Yu Gao and Haiying Chen and Jia Zhou",
year = "2016",
month = "8",
day = "1",
language = "English (US)",
volume = "16",
pages = "2107--2114",
journal = "Current Topics in Medicinal Chemistry",
issn = "1568-0266",
publisher = "Bentham Science Publishers B.V.",
number = "19",

}

TY - JOUR

T1 - Scaffold repurposing of old drugs towards new cancer drug discovery

AU - Chen, Haijun

AU - Wu, Jianlei

AU - Gao, Yu

AU - Chen, Haiying

AU - Zhou, Jia

PY - 2016/8/1

Y1 - 2016/8/1

N2 - As commented by the Nobelist James Black that “The most fruitful basis of the discovery of a new drug is to start with an old drug”, drug repurposing represents an attractive drug discovery strategy. Despite the success of several repurposed drugs on the market, the ultimate therapeutic potential of a large number of non-cancer drugs is hindered during their repositioning due to various issues including the limited efficacy and intellectual property. With the increasing knowledge about the pharmacological properties and newly identified targets, the scaffolds of the old drugs emerge as a great treasure-trove towards new cancer drug discovery. In this review, we summarize the recent advances in the development of novel small molecules for cancer therapy by scaffold repurposing with highlighted examples. The relevant strategies, advantages, challenges and future research directions associated with this approach are also discussed.

AB - As commented by the Nobelist James Black that “The most fruitful basis of the discovery of a new drug is to start with an old drug”, drug repurposing represents an attractive drug discovery strategy. Despite the success of several repurposed drugs on the market, the ultimate therapeutic potential of a large number of non-cancer drugs is hindered during their repositioning due to various issues including the limited efficacy and intellectual property. With the increasing knowledge about the pharmacological properties and newly identified targets, the scaffolds of the old drugs emerge as a great treasure-trove towards new cancer drug discovery. In this review, we summarize the recent advances in the development of novel small molecules for cancer therapy by scaffold repurposing with highlighted examples. The relevant strategies, advantages, challenges and future research directions associated with this approach are also discussed.

KW - Cancer therapeutics

KW - Drug discovery

KW - Drug repurposing

KW - Scaffold repurposing

KW - Structure-activity relationships (SARs)

UR - http://www.scopus.com/inward/record.url?scp=84975682958&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84975682958&partnerID=8YFLogxK

M3 - Article

VL - 16

SP - 2107

EP - 2114

JO - Current Topics in Medicinal Chemistry

JF - Current Topics in Medicinal Chemistry

SN - 1568-0266

IS - 19

ER -