Synthesis, antiproliferative activity, and mechanism of action of a series of 2-{[2E]-3-phenylprop-2-enoylamino}benzamides

Rosaria Maria Pipitone, Giuseppe Daidone, Benedetta Maggio, Stefania Grimaudo, Fabiana Plescia, Maria Valeria Raimondi, Salvatore Plescia, Demetrio Raffa, Stella Maria Cascioferro, Ernest Hamel, Fabiana Plescia, Fabiana Plescia, Fabiana Plescia, Stella Cascioferro, Salvatore Plescia, Demetrio Raffa, Giuseppe Daidone, Maria Valeria Raimondi, Benedetta Maggio, Ruoli BaiAntonietta Di Cristina

Risultato della ricerca: Articlepeer review

25 Citazioni (Scopus)

Abstract

Several new 2-{[2E]-3-phenylprop-2-enoylamino}benzamides 12a-s and 17t-v were synthesized by stirring in pyridine the (E)-3-(2-R1-3-R2-4-R3-phenyl)acrylic acid chlorides 11c-k and 11t-v with the appropriate anthranilamide derivatives 10a-c or the 5-iodo anthranilic acid 13. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). COMPARE analysis, effects on tubulin polymerization in cells and with purified tubulin, and effects on cell cycle distribution for 17t, the most active of the series, indicate that these new antiproliferative compounds act as antitubulin agents
Lingua originaleEnglish
pagine (da-a)2786-2796
Numero di pagine11
RivistaEuropean Journal of Medicinal Chemistry
Volume46
Stato di pubblicazionePublished - 2011

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Fingerprint Entra nei temi di ricerca di 'Synthesis, antiproliferative activity, and mechanism of action of a series of 2-{[2E]-3-phenylprop-2-enoylamino}benzamides'. Insieme formano una fingerprint unica.

Cita questo