Parallel synthesis of "Click" chalcones as antitubulin agents

Maleeruk Utsintong; Alberto Massarotti; Antonio Caldarelli; Sewan Theeramunkong

doi:10.2174/1573406411309040004

Parallel synthesis of "Click" chalcones as antitubulin agents

Maleeruk Utsintong, Alberto Massarotti, Antonio Caldarelli, Sewan Theeramunkong

Dipartimento di Scienze del Farmaco

Risultato della ricerca: Contributo su rivista › Articolo in rivista › peer review

Abstract

It has been shown that some chalcones are able to inhibit tubulin polymerization, giving cytotoxicity and destruction of tumoral vasculature. A library of 180 novel chalcone analogs has been synthesized via click chemistry and screened for their cytotoxicity and tubulin assembly inhibition. 10 out 180 click chalcones displayed low micromolar cytotoxicity but only compound Nf depicted antitubulin activity. While Nf displayed only micromolar potency this result shows click-chalcones may be anti-tubulin agents and validate this strategy to search for novel active chemical entities.

Lingua originale	Inglese
pagine (da-a)	510-516
Numero di pagine	7
Rivista	Medicinal Chemistry
Volume	9
Numero di pubblicazione	4
DOI	https://doi.org/10.2174/1573406411309040004
Stato di pubblicazione	Pubblicato - giu 2013

OSS delle Nazioni Unite

Questo processo contribuisce al raggiungimento dei seguenti obiettivi di sviluppo sostenibile

Accesso al documento

10.2174/1573406411309040004

Altri file e collegamenti

Link to publication in Scopus

Cita questo

@article{a1519f48eb9a47bb8fec780f8cbc69d9,

title = "Parallel synthesis of {"}Click{"} chalcones as antitubulin agents",

abstract = "It has been shown that some chalcones are able to inhibit tubulin polymerization, giving cytotoxicity and destruction of tumoral vasculature. A library of 180 novel chalcone analogs has been synthesized via click chemistry and screened for their cytotoxicity and tubulin assembly inhibition. 10 out 180 click chalcones displayed low micromolar cytotoxicity but only compound Nf depicted antitubulin activity. While Nf displayed only micromolar potency this result shows click-chalcones may be anti-tubulin agents and validate this strategy to search for novel active chemical entities.",

keywords = "Antitubulinic agent, Cancer, Chalcone analogs, Click chemistry, Cytotoxicity, Tubulin",

author = "Maleeruk Utsintong and Alberto Massarotti and Antonio Caldarelli and Sewan Theeramunkong",

year = "2013",

month = jun,

doi = "10.2174/1573406411309040004",

language = "English",

volume = "9",

pages = "510--516",

journal = "Medicinal Chemistry",

issn = "1573-4064",

publisher = "Bentham Science Publishers",

number = "4",

}

TY - JOUR

T1 - Parallel synthesis of "Click" chalcones as antitubulin agents

AU - Utsintong, Maleeruk

AU - Massarotti, Alberto

AU - Caldarelli, Antonio

AU - Theeramunkong, Sewan

PY - 2013/6

Y1 - 2013/6

N2 - It has been shown that some chalcones are able to inhibit tubulin polymerization, giving cytotoxicity and destruction of tumoral vasculature. A library of 180 novel chalcone analogs has been synthesized via click chemistry and screened for their cytotoxicity and tubulin assembly inhibition. 10 out 180 click chalcones displayed low micromolar cytotoxicity but only compound Nf depicted antitubulin activity. While Nf displayed only micromolar potency this result shows click-chalcones may be anti-tubulin agents and validate this strategy to search for novel active chemical entities.

AB - It has been shown that some chalcones are able to inhibit tubulin polymerization, giving cytotoxicity and destruction of tumoral vasculature. A library of 180 novel chalcone analogs has been synthesized via click chemistry and screened for their cytotoxicity and tubulin assembly inhibition. 10 out 180 click chalcones displayed low micromolar cytotoxicity but only compound Nf depicted antitubulin activity. While Nf displayed only micromolar potency this result shows click-chalcones may be anti-tubulin agents and validate this strategy to search for novel active chemical entities.

KW - Antitubulinic agent

KW - Cancer

KW - Chalcone analogs

KW - Click chemistry

KW - Cytotoxicity

KW - Tubulin

UR - https://www.scopus.com/pages/publications/84877974352

U2 - 10.2174/1573406411309040004

DO - 10.2174/1573406411309040004

M3 - Article

SN - 1573-4064

VL - 9

SP - 510

EP - 516

JO - Medicinal Chemistry

JF - Medicinal Chemistry

IS - 4

ER -

Parallel synthesis of "Click" chalcones as antitubulin agents

Abstract

OSS delle Nazioni Unite

Accesso al documento

Altri file e collegamenti

Fingerprint

Cita questo