Given the potent antimicrobial, antiviral, and antitumor activities of many natural products, there is an increasing interest inthe synthesis of new molecules based on natural compound scaffolds. Based on a 2,4-bis(3’-indolyl)imidazole skeleton, two new series of phenylthiazolylindoles and phenylthiazolyl-7-azaindoles were obtained by Hantzsch reaction between substitutedphenylthioamides and the a-bromoacetyl derivatives. Some azaindole derivatives, tested at the National Cancer Instituteagainst a panel of ~60 tumor cell lines derived from nine human cancer cell types, showed inhibitory effects against allcell lines investigated at micromolar to nanomolar concentrations. Two of them exhibited a high affinity for CDK1, with IC50values of 0.41 and 0.85 mm. These promising results will set the foundation for future investigations into the development of anticancer therapies.
|Numero di pagine||10|
|Stato di pubblicazione||Published - 2011|
All Science Journal Classification (ASJC) codes
- Molecular Medicine
- Drug Discovery
- Organic Chemistry