Discovery of JND3229 as a New EGFR Mutant Inhibitor with In Vivo Monodrug Efficacy.

EGFR mutation inducing resistance against third generation EGFR inhibitor drugs is an emerging "unmet clinical need" for nonsmall cell lung cancer patients. The pyrimidopyrimidinone derivative JND3229 was identified as a new highly potent EGFR inhibitor with single digit nM potency. It also exhibited good in vitro and in vivo monodrug anticancer efficacy in a xenograft mouse model of BaF3/EGFR cells.

Four new diterpenoids from the roots of Euphorbia fischeriana.

Four new diterpenoids (1,4,5,9), together with 7 known diterpenoids (2,3,6-8,10,11), were isolated from the roots to Euphorbia fischeriana. On the basis of 1D and 2D NMR, HR-ESI-MS spectroscopic analysis, structures of the new compounds were elucidated as 11β-hydroxy-8,14-epoxy-ent-abieta-13(15)-en-16,12-olide (1), 3,20-dihydroxy-ent-1(10), 15-rosadiene (4), 3,7-dihydroxy-ent-1(10), 15-rosadiene (5), ingenol 6,7-epoxy-3- tetradecanoate (9). The compounds isolated were evaluated for their cytotoxicity against four cancer cell lines (A549, BEL7402, HCT116, and MDA-MB-231).