Symmetrical α-bromoacryloylamido diaryldienone derivatives as a novel series of antiproliferative agents. Design, synthesis and biological evaluation

Bioorganic & Medicinal Chemistry Letters
2010.0

Abstract

In a continuing study of hybrid compounds containing the alpha-bromoacryloyl moiety as potential anticancer drugs, we synthesized a novel series of hybrids 4a-h, in which this moiety was linked to a 1,5-diaryl-1,4-pentadien-3-one system. Many of the conjugates prepared (4b, 4c, 4e and 4g) demonstrated pronounced, submicromolar antiproliferative activity against four cancer cell lines. Moreover, compound 4b induced apoptosis through the mitochondrial pathway and activated caspase-3 in a concentration-dependent manner.

Knowledge Graph

Similar Paper

Symmetrical α-bromoacryloylamido diaryldienone derivatives as a novel series of antiproliferative agents. Design, synthesis and biological evaluation
Bioorganic & Medicinal Chemistry Letters 2010.0
Anticancer activity of novel hybrid molecules containing 5-benzylidene thiazolidine-2,4-dione
European Journal of Medicinal Chemistry 2013.0
Design and synthesis of new coumarin hybrids and insight into their mode of antiproliferative action
Bioorganic & Medicinal Chemistry 2017.0
Design, synthesis and antiproliferative activity of novel heterobivalent hybrids based on imidazo[2,1- b ][1,3,4]thiadiazole and imidazo[2,1- b ][1,3]thiazole scaffolds
European Journal of Medicinal Chemistry 2015.0
Design, synthesis and biological evaluation of [1,2,3]triazolo[4,5-d]pyrimidine derivatives possessing a hydrazone moiety as antiproliferative agents
European Journal of Medicinal Chemistry 2016.0
Design, synthesis and biological evaluation of arylcinnamide hybrid derivatives as novel anticancer agents
European Journal of Medicinal Chemistry 2014.0
Synthesis and biological evaluation of novel 1-aryl, 5-(phenoxy-substituted)aryl-1,4-pentadien-3-one derivatives
MedChemComm 2011.0
Synthesis of novel perillyl–dihydropyrimidinone hybrids designed for antiproliferative activity
MedChemComm 2018.0
Synthesis and antitumor activities of novel dipeptide derivatives derived from dehydroabietic acid
Bioorganic & Medicinal Chemistry Letters 2014.0
Design and synthesis of novel 1,2,3-triazole-pyrimidine hybrids as potential anticancer agents
European Journal of Medicinal Chemistry 2014.0