Discovery of a potent and highly fluorescent sirtuin inhibitor

Y. K. Yoon; M. A. Ali; A. C. Wei; T. S. Choon; A. N. Shirazi; K. Parang

doi:10.1039/c5md00307e

Discovery of a potent and highly fluorescent sirtuin inhibitor

Y. K. Yoon, M. A. Ali, A. C. Wei, T. S. Choon, A. N. Shirazi, K. Parang

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

14 Citations (Scopus)

Abstract

In search for potent sirtuin inhibitors, a series of diversified 1,2-disubstituted benzimidazole analogues were synthesized using a one-pot method. The most potent compound in the series (BZD9L1) was discovered to show high autofluorescence which can be utilized to predict its localization in cells. More importantly, BZD9L1 displayed strong antiproliferative effects against a panel of cancer cells tested. Molecular docking studies also help to explain the observed structure-activity relationship.

Original language	English
Pages (from-to)	1857-1863
Number of pages	7
Journal	MedChemComm
Volume	6
Issue number	10
DOIs	https://doi.org/10.1039/c5md00307e
Publication status	Published - 1 Oct 2015
Externally published	Yes

UN SDGs

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

Access to Document

10.1039/c5md00307e

Cite this

@article{85045ed6447c42e78a8505b18f315607,

title = "Discovery of a potent and highly fluorescent sirtuin inhibitor",

abstract = "In search for potent sirtuin inhibitors, a series of diversified 1,2-disubstituted benzimidazole analogues were synthesized using a one-pot method. The most potent compound in the series (BZD9L1) was discovered to show high autofluorescence which can be utilized to predict its localization in cells. More importantly, BZD9L1 displayed strong antiproliferative effects against a panel of cancer cells tested. Molecular docking studies also help to explain the observed structure-activity relationship.",

author = "Yoon, {Y. K.} and Ali, {M. A.} and Wei, {A. C.} and Choon, {T. S.} and Shirazi, {A. N.} and K. Parang",

year = "2015",

month = oct,

day = "1",

doi = "10.1039/c5md00307e",

language = "English",

volume = "6",

pages = "1857--1863",

journal = "MedChemComm",

issn = "2040-2503",

publisher = "The Royal Society of Chemistry",

number = "10",

}

TY - JOUR

T1 - Discovery of a potent and highly fluorescent sirtuin inhibitor

AU - Yoon, Y. K.

AU - Ali, M. A.

AU - Wei, A. C.

AU - Choon, T. S.

AU - Shirazi, A. N.

AU - Parang, K.

PY - 2015/10/1

Y1 - 2015/10/1

N2 - In search for potent sirtuin inhibitors, a series of diversified 1,2-disubstituted benzimidazole analogues were synthesized using a one-pot method. The most potent compound in the series (BZD9L1) was discovered to show high autofluorescence which can be utilized to predict its localization in cells. More importantly, BZD9L1 displayed strong antiproliferative effects against a panel of cancer cells tested. Molecular docking studies also help to explain the observed structure-activity relationship.

AB - In search for potent sirtuin inhibitors, a series of diversified 1,2-disubstituted benzimidazole analogues were synthesized using a one-pot method. The most potent compound in the series (BZD9L1) was discovered to show high autofluorescence which can be utilized to predict its localization in cells. More importantly, BZD9L1 displayed strong antiproliferative effects against a panel of cancer cells tested. Molecular docking studies also help to explain the observed structure-activity relationship.

UR - http://www.scopus.com/inward/record.url?scp=84943795080&partnerID=8YFLogxK

U2 - 10.1039/c5md00307e

DO - 10.1039/c5md00307e

M3 - Article

AN - SCOPUS:84943795080

SN - 2040-2503

VL - 6

SP - 1857

EP - 1863

JO - MedChemComm

JF - MedChemComm

IS - 10

ER -

Discovery of a potent and highly fluorescent sirtuin inhibitor

Abstract

UN SDGs

Access to Document

Other files and links

Erratum: Discovery of a potent and highly fluorescent sirtuin inhibitor (MedChemComm (2015) 6 (1857-1863))

Cite this