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1.
Org Biomol Chem ; 16(38): 6853-6859, 2018 10 03.
Article in English | MEDLINE | ID: mdl-30065979

ABSTRACT

A straightforward indole synthesis via annulation of C-nitrosoaromatics with conjugated terminal alkynones was realised achieving a simple, highly regioselective, atom- and step economical access to 3-aroylindoles in moderate to good yields. Further functionalizations of indole scaffolds were investigated and an easy way to JWH-018, a synthetic cannabinoid, was achieved.

2.
Bioorg Med Chem ; 19(5): 1649-57, 2011 Mar 01.
Article in English | MEDLINE | ID: mdl-21324703

ABSTRACT

Since activation of p53 in response to cytotoxic stress may have proapoptotic or protective effects depending on the nature of the injury, inhibitors of p53 may have therapeutic interest as modulators of chemotherapy toxicity or efficacy. In an attempt to identify novel p53 inhibitors, a quality collection of compounds structurally related to pifithrin-ß were designed and synthesized as potential inhibitors of p53. The biochemical and biological evaluations supported that compounds of the tetrahydrobenzothiazole series were inhibitors of the p53 transcriptional activity and were effective in enhancing paclitaxel-induced apoptosis. In contrast, in spite of the increased cytotoxic potency, selected compounds of the benzothiazole series were not able to modulate the transcriptional activity of p53, as indicated by lack of change of p21 expression. The therapeutic interest of the compounds of the former series in combination with taxanes was confirmed in a human tumor xenograft model.


Subject(s)
Antineoplastic Agents , Benzothiazoles/chemical synthesis , Benzothiazoles/pharmacology , Ovarian Neoplasms/drug therapy , Toluene/analogs & derivatives , Tumor Suppressor Protein p53/antagonists & inhibitors , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/chemistry , Antineoplastic Agents/pharmacology , Benzothiazoles/chemistry , Cell Line, Tumor , Disease Models, Animal , Female , Gene Expression Regulation/drug effects , Humans , Inhibitory Concentration 50 , Toluene/chemical synthesis , Toluene/chemistry , Toluene/pharmacology , Transplantation, Heterologous
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