Synthesis and biological activities of topopyrones

Paul A. Zaleski; Rumit Maini; Simon J. Leiris; Mark A. Elban; Sidney Hecht

doi:10.1021/np200777z

Synthesis and biological activities of topopyrones

Paul A. Zaleski, Rumit Maini, Simon J. Leiris, Mark A. Elban, Sidney Hecht

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

17 Scopus citations

Abstract

Structure-activity studies were employed to investigate the stabilization of DNA-topoisomerases I and II covalent binary complexes by topopyrone analogues. The synthesis of five new topopyrone derivatives and study of their ability to stabilize DNA-topoisomerase I and DNA-topoisomerase II covalent binary complexes are described. The biochemical assays suggest that the orientation of the fused 1,4-pyrone ring and halogen substituents contribute importantly to the overall potency of the topopyrones as topoisomerase poisons.

Original language	English (US)
Pages (from-to)	577-585
Number of pages	9
Journal	Journal of Natural Products
Volume	75
Issue number	4
DOIs	https://doi.org/10.1021/np200777z
State	Published - Apr 27 2012

ASJC Scopus subject areas

Analytical Chemistry
Molecular Medicine
Pharmacology
Pharmaceutical Science
Drug Discovery
Complementary and alternative medicine
Organic Chemistry

Access to Document

10.1021/np200777z

Cite this

@article{aded74648feb4a4183e2232acd8bff36,

title = "Synthesis and biological activities of topopyrones",

abstract = "Structure-activity studies were employed to investigate the stabilization of DNA-topoisomerases I and II covalent binary complexes by topopyrone analogues. The synthesis of five new topopyrone derivatives and study of their ability to stabilize DNA-topoisomerase I and DNA-topoisomerase II covalent binary complexes are described. The biochemical assays suggest that the orientation of the fused 1,4-pyrone ring and halogen substituents contribute importantly to the overall potency of the topopyrones as topoisomerase poisons.",

author = "Zaleski, {Paul A.} and Rumit Maini and Leiris, {Simon J.} and Elban, {Mark A.} and Sidney Hecht",

year = "2012",

month = apr,

day = "27",

doi = "10.1021/np200777z",

language = "English (US)",

volume = "75",

pages = "577--585",

journal = "Journal of Natural Products",

issn = "0163-3864",

publisher = "American Chemical Society",

number = "4",

}

TY - JOUR

T1 - Synthesis and biological activities of topopyrones

AU - Zaleski, Paul A.

AU - Maini, Rumit

AU - Leiris, Simon J.

AU - Elban, Mark A.

AU - Hecht, Sidney

PY - 2012/4/27

Y1 - 2012/4/27

N2 - Structure-activity studies were employed to investigate the stabilization of DNA-topoisomerases I and II covalent binary complexes by topopyrone analogues. The synthesis of five new topopyrone derivatives and study of their ability to stabilize DNA-topoisomerase I and DNA-topoisomerase II covalent binary complexes are described. The biochemical assays suggest that the orientation of the fused 1,4-pyrone ring and halogen substituents contribute importantly to the overall potency of the topopyrones as topoisomerase poisons.

AB - Structure-activity studies were employed to investigate the stabilization of DNA-topoisomerases I and II covalent binary complexes by topopyrone analogues. The synthesis of five new topopyrone derivatives and study of their ability to stabilize DNA-topoisomerase I and DNA-topoisomerase II covalent binary complexes are described. The biochemical assays suggest that the orientation of the fused 1,4-pyrone ring and halogen substituents contribute importantly to the overall potency of the topopyrones as topoisomerase poisons.

UR - http://www.scopus.com/inward/record.url?scp=84860316468&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84860316468&partnerID=8YFLogxK

U2 - 10.1021/np200777z

DO - 10.1021/np200777z

M3 - Article

C2 - 22462811

AN - SCOPUS:84860316468

SN - 0163-3864

VL - 75

SP - 577

EP - 585

JO - Journal of Natural Products

JF - Journal of Natural Products

IS - 4

ER -

Synthesis and biological activities of topopyrones

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this