Antitumour Activity of Chitosan Hydrogen Selenites

Chitosans reacted with selenious acid to prepare chitosan hydrogen selenites, which were found to be growth-inhibitory against sarcoma 180 solid tumor. The results indicated that the activity also depended on the molecular weight of chitosan supports.

CARBOXYMETHYLPACHYMAN(Ⅰ),A NEW WATER SOLUBLE POLYSACCHARIDE WITH MARKED ANTITUMOUR ACTIVITY

Carboxymethylpachyman(Ⅰ)was formed by carboxymethylation of β-pachyman.The antitumour activity of carboxymethylpachyman(Ⅰ)against S_(180)、EAC、 MA、U_(14)was measured.The structure of carboxymethylpachyman(Ⅰ)was proved by IR ^(13)CNMR spectroscopy.

Synthesis, Characterization and in vitro Antitumour Activity of the Di-n-butyltin(IV) Complexes of Some Arylhydroxamates

Fourteen new di n butyltin(IV) complexes of hydroxamic acids of the formula Bu 2 SnL 2 (HL=hydroxamic acids) were synthesized by the reaction of Bu 2 SnO and hydroxamic acids in dry toluene and ethanol media. The compounds were characterized by elemental analyses, molecular weight, IR and 1 H NMR spectroscopy. The results indicate that n Bu 2 SnL 2 have distorted trans octahedral structure. The antitumor activity in vitro against human A 549 tumor cells and P388 leukemia was presented, and their structure activity relationship was discussed.

Activating Effect of Staphylococcal Enterotoxins

The effect of enterotoxins is to induce the production of endogenous IF. St. aureus enteropathogenic proteins (enterotoxins) possess an antitumour effect. After intraperitoneal inoculation, they decrease the size and, in some cases, prevent the development of the human hypernephroma in the cheek pouch of golden hamsters. The effect of enteropathgenic proteims may possibly consist in inducing the production of endogenous immune interferon which activates the host immune system and enhances the rejection of heterologous tumour cells.

Synthesis, Characterization and Biological Activity of Diorganotin（IV） Complexes of N-（3,5-Dibromosalicylidene）-α-amino Acid

The diorganotin（Ⅳ） complexes of N-（3,5-dibromosalicylidene）-α-amino acid, R2Sn（2-O-3,5-Br2C6H2CH= NCHRCOO）（where R=H, Me, i-Pr, Bz; R＇=n-Bu, Cy）, were synthesized by the reactions of diorganotin dichlorides with in situ formed potassium salt of N-（3,5-dibromosalicylidene）-α-amino acid and characterized by elemental analysis, IR and NMR （^1H, ^13C and ^119Sn） spectra. The crystal structures of n-Bu2Sn（2-O-3,5-Br2C6H2CH= NCHRCOO）（R=i-Pr, Bz） and Cy2Sn（2-O-3,5-Br2C6H2CH=NCHRCOO）（R=Me, Bz） were determined by X-ray single crystal diffraction and showed that the tin atoms are in a distorted trigonal bipyramidal geometry to form five- and six-membered chelate rings with the tridentate ligand. Bioassay results indicated that the compounds possess better in vitro antitumour activity against three human tumour cell lines, HeLa, CoLo205 and MCF-7, than cis-platin and moderate anti-bacterial activity against two bacteria, E. coli and S. aureus.

Design, Synthesis and Antitumor Activity of Novel Indolin-2-one Derivatives Containing 4-Thiazolidinone Moiety

A series of novel indolin-2-one derivatives containing 4-thiazolidinone moiety（7a--7r） were synthesized and evaluated for their in vitro antitumour activities against MDA-MB-231 （human breast cancer）, H460（human lung cancer） and HT-29（human colon cancer） cell lines by standard 3-（4,5-dimethylthiazae-2-yl）-2,5-diphenyltetrazo- lium bromide（MTT） assay. Representative compounds（Td, 7k, 7m, 7p） with higher cytotoxicity were further examined against one normal cell line（WI-38, human fetal lung fibroblasts）. The preliminary investigation shows that most of the compounds display moderate to excellent potency and high selectivity against different human cancer cell lines. In particular, the most potent compound 7m shows promising cytotoxicity against MDA-MB-231, H460 and HT-29 cell lines with IC5o values of 0.78, 0.056 and 0.018 μmol/L, respectively. The potency is much higher than that of Sunitinib（IC50=3.46 μmol/L against MDA-MB-231, IC50=2.59 μmol/L against H460, IC50=1.50 μmol/L against HT-29） by 4.4, 46.3 and 83.3 fold.