Five new mexicanolide-type limonoids,heytrijunolides A-E(1-5)were isolated from the branches and leaves of Heynea trijuga.The structures of these new compounds were elucidated on the basis of extensive spectroscopic analysis.Compound 3 showed weak cytotoxicity against HL-60,SMMC-7721 and A-549 human tumor cell lines with the IC50 values of 21.88,20.66 and 12.70μM,respectively.
Two new tirucallane triterpenoids,2a-ethoxy-2,3-secotirucalla-2,29-epoxy-7-ene-23-oxo-3-oic acid(1)and(23E)-2a-hydroxytirucalla-7,23,25-triene-3-one(2),along with the known 2,3-secotirucalla-2,3;2,29-diepoxy-7-ene-3,23-dione(3),were isolated from the leaves and twigs of Aphanamixis grandifolia.Their structures were elucidated by extensive NMR and MS data,and compound 3 was further confirmed by X-ray crystal diffraction analysis.Antimicrobial activities and insecticidal activities of these three compounds were also evaluated.Compound 1 showed good antimicrobial activity against Staphylococcus aureus with the MIC value of 1.56μg/mL,while compounds 1 and 2 showed insecticidal activity at 100 ppm,with the corrected mortality 79.1%and 60.6%,respectively.
Xiao-Ying WANGGui-Hua TANGChun-Mao YUANYu ZHANGLi HOUQing ZHAOXiao-Jiang HAOHong-Ping HE
We designed a series of 2-methylpyrimidine derivatives as new BCR-ABL inhibitors using scaffold-hopping strategy.These synthetic compounds exhibited significant inhibition against a broad spectrum of Bcr-Abl mutants including the gatekeeper T315I mutant.Compound 7u showed very potent kinase inhibitory activities against Bcr-Abl WT,Bcr-Abl E255K,Bcr-Abl Q252H,Bcr-Abl G250E and Bcr-Abl T315I,with IC50 values of 0.13 nM,0.17 nM,0.24 nM,0.19 nM and 0.65μM,respectively.This compound also displayed anti-proliferation activity against K562 cell line with an IC50 value of 1.1 nM,thus representing a new lead for further optimization.
ZOU DingBiaoQIU YaTaoTU ZhengChaoLIAO ChenZhongLUO JinFengMENG QingQingYAO RiShengLI ZhengJIANG Sheng
Sixβ-carboline alkaloids including three new ones,trifilines A-C(1-3)were isolated from Trigonostemon filipes,along with a newβ-carboline alkaloid,trigonoine C(7)isolated from Trigonostemon lii.Their structures were elucidated by extensive spectroscopic techniques.Trifilines A(1)and B(2)showed weak anti-HIV-1 activity with EC50 values of 54.61μg/mL and 9.75μg/mL,along with TI(Therapeutic index)values of 1.52 and 1.42,respectively.This is the first time to report the chemical constituents of Trigonostemon filipes.
