RESUMEN
Secocycloartanes are a class of triterpenoids with novel structures showing anti-HIV and antitumor activities. This review summarized the structures, bioactivities and plant distribution of secocycloartane triterpenoids reported from plants but Schisandraceae in recent years to provide a basis for further study of this type of compound and the discovery of new drugs.
RESUMEN
Due to their role in the inhibition of non nucleoside reverse transcriptase, 4,5,6,7-Tetrahydro- 5-methylimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)-ones (TIBO) derivatives present a significant importance as a potent chemotherapeutic agent against the AIDS disease. In this work, we report our attempt to find out the other factors required in quantitative structure-activity relationship for a set of 89 TIBO derivatives. In vitro Anti HIV activity of TIBO derivatives logIC50 expressed as log1/C values were considered as a biological activity parameter. The QSAR study of the dataset of 89 TIBO derivatives was performed using different parameters namely Topological, physicochemical, hydrophobic descriptors and indicator parameters. Multiple regression analysis performed to obtain QSAR model and to capture the descriptor other than the logP. The QSAR study highlights the logP, Is and surface area grid (SAG) descriptors, that affect the anti HIV activity of these TIBO derivatives. SAG is found as the cofactor working with hydrophobicity of TIBO derivatives. Eventually, the study provides a strong foundation to design new and more potent inhibitors of HIV-1 RT.