538-60-3Relevant articles and documents
Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo
Yan, Jun,Chen, Jie,Zhang, Shun,Hu, Jinhui,Huang, Ling,Li, Xingshu
, p. 5264 - 5283 (2016/07/06)
Twenty-nine novel indole-chalcone derivatives were synthesized and evaluated for antiproliferative activity. Among them, 14k exhibited most potent activity, with IC50 values of 3-9 nM against six cancer cells, which displayed a 3.8-8.7-fold increase in activity when compare with compound 2. Further investigation revealed 14k was a novel tubulin polymerization inhibitor binding to the colchicine site. Its low cytotoxicity toward normal human cells and nearly equally potent activity against drug-resistant cells revealed the possibility for cancer therapy. Cellular mechanism studies elucidated 14k arrests cell cycle at G2/M phase and induces apoptosis along with the decrease of mitochondrial membrane potential. Furthermore, good metabolic stability of 14k was observed in mouse liver microsomes. Importantly, 14k and its phosphate salt 14k-P inhibited tumor growth in xenograft models in vivo without apparent toxicity, which was better than the reference compound CA-4P and 2. In summary, 14k deserves consideration for cancer therapy.
Method and compositions for identifying anti-HIV therapeutic compounds
-
, (2008/06/13)
Methods are provided for identifying anti-HIV therapeutic compounds substituted with carboxyl ester or phosphonate ester groups. Libraries of such compounds are screened optionally using the novel enzyme GS-7340 Ester Hydrolase. Compositions and methods relating to GS-7340 Ester Hydrolase also are provided.
Selective phosphorylation on primary alcohols of unprotected polyols
Ladame, Sylvain,Claustre, Samantha,Willson, Michele
, p. 37 - 47 (2007/10/03)
The triad tribenzylphosphite-iodine-pyridine offers a general selective method for phosphorylation reactions of primary alcohols of unprotected α-diols and polyols. A mechanistic study by 31P NMR allowed to evidence the formation, from iododibenzyl phosphate and pyridine, of a very reactive pyridinium salt intermediate. This analysis shows that pyridine behaves as a covalent catalyst like DMAP in acylation reactions from acylchloride. Due to its steric hindrance and high reactivity, this species appears to be the efficient selective phosphorylation reagent but leads to dibenzylphosphoric esters. Under mild conditions, the cleavage of benzyl groups gives monoester phosphoric acid.
