Novel Microtubule-Targeting 7-Deazahypoxanthines Derived from Marine Alkaloid Rigidins with Potent in Vitro and in Vivo Anticancer Activities
JOURNAL OF MEDICINAL CHEMISTRY
2016; 59 (1): 480–85
Docking studies of tubulin-targeting C2-substituted 7-deazahypoxanthine analogues of marine alkaloid rigidins led to the design and synthesis of compounds containing linear C2-substituents. The C2-alkynyl analogue was found to have double- to single-digit nanomolar antiproliferative IC50 values and showed statistically significant tumor size reduction in a colon cancer mouse model at nontoxic concentrations. These results provide impetus and further guidance for the development of these rigidin analogues as anticancer agents.
View details for DOI 10.1021/acs.jmedchem.5b01426
View details for Web of Science ID 000368564400034
View details for PubMedID 26641132
View details for PubMedCentralID PMC4950951