Synthesis and Biological Activity of Some Bile Acid-Based Camptothecin Analogues
作者:Xingnuo Li、Tengfei Zhao、Dongping Cheng、Chu Chu、Shengqiang Tong、Jizong Yan、Qing-Yong Li
DOI:10.3390/molecules19033761
日期:——
In an effort to decrease the toxicity of camptothecin (CPT) and improve selectivity for hepatoma and colon cancer cells, bile acid groups were introduced into the CPT 20 or 10 positions, resulting in the preparation of sixteen novel CPT-bile acid analogues. The compounds in which a bile acid group was introduced at the 20-hydroxyl group of CPT showed better cytotoxic selectivity for human hepatoma and colon cancer cells than for human breast cancer cells. Fluorescence microscopy analysis demonstrated that one compound (E2) entered human hepatoma cells more effectively than it did human breast cancer cells. Compound G4 exhibited the best anti-tumour activity in vivo. These results suggested that introduction of a bile acid group at the 20-position of CPT could decrease toxicity in vivo and improve selectivity for hepatoma cells.
Radio-opaque compounds, compositions containing same and methods of their synthesis and use
申请人:Pathak P. Chandrashekhar
公开号:US20050036946A1
公开(公告)日:2005-02-17
Radio-opaque biodegradable compositions are formed by modifying terminal groups of synthetic and natural biodegradable polymers such as polylactones with iodinated moieties. The biodegradable property of the compositions renders them suitable for use in medical field such as drug delivery, imaging. Compounds disclosed in this invention exist as neat liquid. Certain compositions disclosed in this invention form hydrophobic iodine rich domains when dissolved in water, such domains provide better contrasting properties as well as ability to dissolve hydrophobic bioactive drugs. Certain iodinated moieties disclosed in the invention are capable of cross linking natural proteins in situ in presence of suitable catalysts and co-catalysts.
Electrical Communication between Glucose Oxidase and Electrodes Mediated by Phenothiazine-Labeled Poly(ethylene oxide) Bonded to Lysine Residues on the Enzyme Surface
poly(ethylene oxide) (PT-PEO)) capable of direct electrical communication with electrodes is synthesized by covalently modifying PT-PEO to lysine residues on the enzyme surface. The length of the PEO chain and the number of PT groups are systematically altered. After the PT-PEO modification, all the hybrids maintain more than 50% of enzyme activity relative to that of native GOx, although loss of the activity
We have developed the first green-light-emitting, spontaneously blinking fluorophore (SBF), HEtetTFER.
我们已经开发出第一种绿光发射、自发闪烁的荧光物质(SBF),HEtetTFER。
Protein crosslinkers, crosslinking methods and applications thereof
申请人:Pathak Chandrashekhar P.
公开号:US20070248567A1
公开(公告)日:2007-10-25
Some aspects of this disclosure relate to a method for crosslinking a biological fluid comprising combining a biological fluid with a crosslinker to covalently crosslink proteins endogenous to the biological fluid to form a crosslinked gel. Examples of a biological fluid are blood, plasma, or serum.