1314082-92-2Relevant articles and documents
Synthesis and Antitumor Activity of 3-(2-Phenyl-1,3-thiazol-4-yl)-1H-indoles and 3-(2-Phenyl-1,3-thiazol-4-yl)-1H-7-azaindoles
Diana, Patrizia,Carbone, Anna,Barraja, Paola,Montalbano, Alessandra,Parrino, Barbara,Lopergolo, Alessia,Pennati, Marzia,Zaffaroni, Nadia,Cirrincione, Girolamo
, p. 1300 - 1309 (2012/05/05)
Given the potent antimicrobial, antiviral, and antitumor activities of many natural products, there is an increasing interest in the 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 substituted phenylthioamides and the α-bromoacetyl derivatives. Some azaindole derivatives, tested at the National Cancer Institute against a panel of ～60 tumor cell lines derived from nine human cancer cell types, showed inhibitory effects against all cell lines investigated at micromolar to nanomolar concentrations. Two of them exhibited a high affinity for CDK1, with IC50 values of 0.41 and 0.85μM. These promising results will set the foundation for future investigations into the development of anticancer therapies. Marine mining: Given the promise of marine-derived bioactive indole alkaloids, we synthesized a series of phenylthiazolylindoles and phenylthiazolyl-7-azaindoles, and evaluated their antitumor activity against a panel of 60 cancer cell lines. Some derivatives showed IC50 values in the micromolar to nanomolar range.
