144693-66-3Relevant articles and documents
Design, synthesis and evaluation of antiproliferative activity of melanoma-targeted histone deacetylase inhibitors
Raji, Idris,Ahluwalia, Kabir,Oyelere, Adegboyega K.
, p. 744 - 749 (2017)
The clinical validation of histone deacetylase inhibition as a cancer therapeutic modality has stimulated interest in the development of new generation of potent and tumor selective histone deacetylase inhibitors (HDACi). With the goal of selective delivery of the HDACi to melanoma cells, we incorporated the benzamide, a high affinity melanin-binding template, into the design of HDACi to generate a new series of compounds 10a-b and 11a-b which display high potency towards HDAC1 and HDAC6. However, these compounds have attenuated antiproliferative activities relative to the untargeted HDACi. An alternative strategy furnished compound 14, a prodrug bearing the benzamide template linked via a labile bond to a hydroxamate-based HDACi. This pro-drug compound showed promising antiproliferative activity and warrant further study.
Synthesis and characterization of poly(phenylacetylenes) featuring activated ester side groups
Pauly, Anja C.,Theato, Patrick
experimental part, p. 211 - 224 (2011/09/16)
Four monomers based on 4-ethynylbenzoic acid have been synthesized, one of those featuring an activated ester. With the metathesis catalytic system WCl6/Ph4Sn, these acetylenic monomers could successfully be polymerized yielding conjugated polymers with molecular weights of around 10,000 to 15,000 g/mol and molecular weight distributions Mw/M n ≤ 2.1. Also the copolymerization of phenylacetylene or methyl 4-ethynylbenzoate with pentafluorophenyl 4-ethynylbenzoate as reactive unit was conducted. Polymer analogous reactions of the reactive polymers and copolymers with amines have been investigated and it was found that poly(pentafluorophenyl 4-ethynylbenzoate) featured a significant reactivity, such that reactions proceeded quantitatively even with aromatic amines. Moreover the UV-Vis spectra of the activated ester based polymer before and after conversion with aliphatic amines showed a change, indicating an effect on the conjugated backbone of the polymers. Copyright