Synthesis and cytotoxic activity of heterocycle-substituted phthalimide derivatives

<正>A series of heterocycle-substituted phthalimide derivatives were synthesized.Structurally diverse derivatives with heterocyclic rings,including furan,imidazo[1,2-a]pyridine,1,3,4-thiadiazine,imidazo[2,1-b][1,3,4]thiadiazine,pyrazole,1,2,4-triazolo[3,4- b][1,3,4]thiadiazine,thiazole and thiazoline,were obtained by the reactions ofα-bromoketone intermediate with various nucleophiles containing oxygen,nitrogen and sulfur atom.Their cytotoxic activity was also evaluated against five human cancer cell lines in vitro.     

Syntheses of haptens and hapten-protein conjugates for insecticide propoxur and cyhalothrin

A facile procedure was described for the hapten design of the N-methylcarbamate insecticide propoxur.Two new haptens of propoxur(hapten 1a and hapten 1b) were synthesized by introducing appropriate spacers in the pesticide aromatic moiety of the analyte molecular structure.First,the propoxur reacted with nitric acid to yield the intermediate product.Then hapten 1a was prepared via the reduction of the intermediate product,and hapten 1b was formed by the acylation of hapten 1a with succinic anhydride.In addi...     

A new sulfated triterpenoid from the bark of Zygophyllum fabago L.

<正>A new sulfated triterpenoid,3β,24-dihydroxyurs-20-ene-24-O-sulphonyl-28-oic acid(fabagoin.1) was isolated from the barks of Zygophyllum fabago L.Its structure was elucidated on the basis of spectroscopic data.     

A new ent-labdane diterpenoid from Andrographis paniculata

<正>A new ent-labdane diterpenoid,19-O-β-D-glucopyranosyl-ent-labda-8(17),13-dien-15,16,19-triol,together with six known ent-labdane diterpenoids,was isolated from the aerial parts of Andrographis paniculaia.The structure of the new compound was elucidated by extensive spectral analysis.     

A New Indole Alkaloid from Limonia Crenulata

Limonia crenulata Roxb. (Rutaceae), a small tree widely distributed in dry warm regions of southeastern Asia, has been reported to have antiepileptic, purgative and sudorific effects and is used for colic trouble and cardialgia1. Various parts of this plant have been employed in indigenous medicine. Our investigation on its stems led to the isolation of one new alkaloid, crenulatine 1, together with three known ones, 4-methoxy-6- hydroxy-1-methyl-2-quinolone2, N-benzoyltyramine methyl ether2,…     

First total synthesis of eudistalbin A

<正>Eudistalbin A was isolated from marine tunicate eudistoma album and possess cytotoxic activity(ED_(50)3.2μg/mL) in vitro against the growth of KB human buccal carinoma cells.The synthetic eudistalbin A showed potent inhibitory activity against the breast carcinoma cell line MDA-231 with an IC_(50) value of 2.1μmol/L using the metabolic assay MTT.All structures of new compounds were confirmed by ~1H NMR,~(13)C NMR,HRMS and optical rotation.     

人血胃泌素的毛细管电泳定量测定

用自制涂渍毛细管柱在HPE-100毛细管电泳仪(Bio-Rad USA)上以区带电泳模式对胃泌素作定量测定。苯甲酸被用作内标。用胃泌素和苯甲酸的峰高比对胃泌素浓度作图,在1～8 mg/L内测得其浓度标准曲线,相关系数达0.9994,截距接近于0,结果优于用峰面积得到的数值。在同种浓度下,5次测量迁移时间的相对标准偏差(RSD)小于0.7%,不同浓度下的24次平行操作的相应值在0.9%～1.1%之间。胃泌素测定的绝对量为0.38pg,即3.6×10~(-15)mol。     

一个亲脂的环腺苷酸类似物的合成及其活性

基于高度亲脂的分子可能增强对神经细胞膜的渗透力的设想,合成了一种新的环腺苷酸的类似物2'-O-oleoy1-2-(?)aza-adenosine 3',5'-cyclic phosphate(3),发现在10~(-3),10~(-4)和10~(-5)M时,该化合物对小鼠神经胶质癌组织培养细胞的杀灭率分别是97%,86%和60%。     

Direct observation of the autophosphorylation of insulin receptor kinase by mass spectrometry

The catalytic and signaling activities of insulin receptor kinase(IRK)are regulated by the autophosphorylation of three tyrosine residues in a cytoplasmic protein-tyrosine kinase domain at Tyro 1158,Tyro 1162 and Tyro 1163.In this study,time-course of the auphosphorylation of the core kinase(residues 978-1283)from IRK was directly investigated by online electrospray ionization mass spectrometry.It is found that two tyrosine residues were phosphorylated in reaction time range of 30 min.This study implies ...     

A colorimetric and fluorometric fluoride sensor based on a BODIPY-phenol conjugate

A boradiazaindacenes (BODIPY)-phenol conjugate,1,can act as a colorimetric and fluorometric sensor for sensitive and se-lective measurement of F-over AcO-and H2PO-4 in CH3CN. Sensor 1 gives response to F-in a 1:1 ratio via the deprotonation of the phenolic OH proton,which results in color change from pale yellow to light green and quenching of bright green fluo-rescence.