2. Academic Validation
  3. Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors

Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-amino 5-aryl thiophenes as a new class of tubulin inhibitors

  • J Med Chem. 2006 Oct 19;49(21):6425-8. doi: 10.1021/jm060804a.
Romeo Romagnoli 1,  Pier Giovanni Baraldi,  Vincent Remusat,  Maria Dora Carrion,  Carlota Lopez Cara,  Delia Preti,  Francesca Fruttarolo,  Maria Giovanna Pavani,  Mojgan Aghazadeh Tabrizi,  Manlio Tolomeo,  Stefania Grimaudo,  Jan Balzarini,  Mary Ann Jordan,  Ernest Hamel
Affiliations

Affiliation

  • 1 Dipartimento di Scienze Farmaceutiche, Università di Ferrara, 44100 Ferrara, Italy. [email protected]
PMID: 17034150 DOI: 10.1021/jm060804a
Abstract

2-(3',4',5'-Trimethoxybenzoyl)-3-amino-5-aryl/heteroaryl thiophene derivatives were synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. SARs were elucidated with various substitutions on the aryl moiety 5-position of the thienyl ring. Substituents at the para-position of the 5-phenyl group showed antiproliferative activity in the order of F=CH(3) > OCH(3)=Br=NO(2) > CF(3)=I > OEt. Several of these compounds led to arrest of HL-60 cells in the G2/M phase of the cell cycle and induction of Apoptosis.

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