Pyrazole ring-containing isolongifolanone derivatives as potential CDK2 inhibitors: Evaluation of anticancer activity and investigation of action mechanism.

Isolongifolanone is a high value-added sustainable natural product. Recent studies have demonstrated that isolongifolanone possesses anticancer activities. In this study, a series of novel pyrazole ring-containing isolongifolanone derivatives was designed, synthesized, and their anti-proliferative activities in three cancer cell lines were evaluated.

Novel camphor-based pyrimidine derivatives induced cancer cell death through a ROS-mediated mitochondrial apoptosis pathway.

A series of novel camphor-based pyrimidine derivatives (3a-3x) have been synthesized; their structures were determined by using conventional methods and compound 3f was further confirmed through single crystal XRD analysis. The cytotoxic activity of the target compounds against a panel of human normal (GES-1) and cancer cell lines (MDA-MB-231, RPMI-8226, A549) was evaluated by MTS assay. Here we found that compound 3f exhibited the strongest anti-tumor activity, comparable to that of etoposide, and had much lower cytotoxicity to normal GES-1 cells (IC > 50 μM) than the reference drug (IC = 8.

Synthesis and antitumor activity of isolongifoleno[7,8-d]thiazolo[3,2-a]pyrimidine derivatives via enhancing ROS level.

A series of novel isolongifoleno[7,8-d]thiazolo[3,2-a]pyrimidine derivatives (4a-4x) were synthesized from isolongifolanone according fragment-based design strategy, and their anticancer activity against human aortic smooth muscle cells (HASMC), human breast cancer (MCF-7) cells, human cervical cancer (HeLa) cells, and human liver cancer (HepG2) cells were investigated. Results of the anticancer activity illustrated that most of the compounds showed potent antitumor activity and compound 4i proved to be the most active derivative with IC values of 0.33 ± 0.