Acridine Based N-Acylhydrazone Derivatives as Potential Anticancer Agents: Synthesis, Characterization and ctDNA/HSA Spectroscopic Binding Properties

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15640%2F22%3A73618813" target="_blank" >RIV/61989592:15640/22:73618813 - isvavai.cz</a>

Result on the web

<a href="https://www.mdpi.com/1420-3049/27/9/2883" target="_blank" >https://www.mdpi.com/1420-3049/27/9/2883</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.3390/molecules27092883" target="_blank" >10.3390/molecules27092883</a>

Result language

angličtina

Original language name

Acridine Based N-Acylhydrazone Derivatives as Potential Anticancer Agents: Synthesis, Characterization and ctDNA/HSA Spectroscopic Binding Properties

Original language description

A series of novel acridine N‐acylhydrazone derivatives have been synthesized as potential topoisomerase I/II inhibitors, and their binding (calf thymus DNA—ctDNA and human serum albumin—HSA) and biological activities as potential anticancer agents on proliferation of A549 and CCD‐18Co have been evaluated. The acridine‐DNA complex 3b (‐F) displayed the highest Kb value (Kb = 3.18 × 103 M−1). The HSA‐derivatives interactions were studied by fluorescence quenching spectra. This method was used for the calculation of characteristic binding parameters. In the presence of warfarin, the binding constant values were found to decrease (KSV = 2.26 M−1, Kb = 2.54 M−1), suggesting that derivative 3a could bind to HSA at Sudlow site I. The effect of tested derivatives on metabolic activity of A549 cells evaluated by the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐ diphenyltetrazolium bromide or MTT assay decreased as follows 3b (‐F) &gt; 3a(‐H) &gt; 3c(‐Cl) &gt; 3d(‐Br). The derivatives 3c and 3d in vitro act as potential dual inhibitors of hTopo I and II with a partial effect on the metabolic activity of cancer cells A594. The acridine‐benzohydrazides 3a and 3c reduced the clonogenic ability of A549 cells by 72% or 74%, respectively. The general results of the study suggest that the novel compounds show potential for future development as anticancer agents.

Czech name

—

Czech description

—

Type

J_imp - Article in a specialist periodical, which is included in the Web of Science database

CEP classification

—

OECD FORD branch

10608 - Biochemistry and molecular biology

Project

—

Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2022

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

MOLECULES

ISSN

1420-3049

e-ISSN

—

Volume of the periodical

27

Issue of the periodical within the volume

9

Country of publishing house

CH - SWITZERLAND

Number of pages

31

Pages from-to

"nečíslováno"

UT code for WoS article

000796147400001

EID of the result in the Scopus database

2-s2.0-85129860812