Potent inhibition of tributyltin (TBT) and triphenyltin (TPT) against multiple UDP-glucuronosyltransferases (UGT): A new potential mechanism underlying endocrine disrupting actions.

Organotin compounds (OTs) act as potent endocrine disruptors that are often found in polluted food and water. UDP-glucuronosyltransferases (UGTs) are responsible for termination of multiple endogenous hormones. This study was conducted to investigate the inhibitory effects of two tri-submitted OTs tributyltin (TBT) and triphenyltin (TPT), against activities of UGTs.

Effects of single and double bonds in linkers on colorimetric and fluorescent sensing properties of polyving akohol grafting rhodamine hydrazides.

Two rhodamine derivatives, N-mono-maleic acid amide-N'-rhodamine B hydrazide (MRBH) and N-mono-succinic acid amide-N'-rhodamine 6G hydrazide (SR6GH), were synthesized by amidation with maleic anhydride (MAH), succinic anhydride (SAH) and rhodamine B hydrazide, rhodamine 6G hydrazide, which were identified by FTIR, (1)H NMR and elemental analysis. Two water-soluble fluorescent materials (PVA-MRBH and PVA-SR6GH) were prepared via esterification reaction with N-mono-maleic acyl chloride amide-N'-rhodamine B hydrazide (MRBHCl) or N-mono-maleic acyl chloride amide-N'-rhodamine 6G hydrazide (SR6GHCl) and poly(vinyl alcohol) (PVA) in DMSO solution. The sensing behaviors of PVA-MRBH and PVA-SR6GH were explored by recording the fluorescence spectra in completely aqueous solution.

Synthesis and biological evaluation of novel 1,6-diaryl pyridin-2(1H)-one analogs.

A series of 1,6-diaryl pyridin-2(1H)-one analogs were designed and synthesized via consecutive Chan-Lam coupling and Suzuki coupling. These novel compounds were evaluated for their antiproliferative activity against two tumor cell lines (SKOV-3 and HepG2). Compounds 1b, 1c, 1e and 1f displayed comparable in vitro cytotoxicity with taxol, while their in vivo antitumor activity was less effective than taxol.

Synthesis and in vitro cytotoxic evaluation of novel N-(3,4,5-trimethoxyphenyl)pyridin-2(1H)-one derivatives.

A series of novel [Formula: see text]-(3,4,5-trimethoxyphenyl)pyridin-2([Formula: see text])-one derivatives were designed, synthesized, and evaluated for their in vitro cytotoxicity against human colon cancer cells HCT-116. The key steps involved consecutive Chan-Lam- and Buchwald-Hartwig couplings. Most of these C-6 substituted pyridone derivatives showed moderate antiproliferative activity.