|别名||吖啶酮 ;茚酮,氮蒽酮，9(10H)吖啶酮;9(10h)-acridinone 9,10-Dihydro-9-oxoacridine|
|个人防护设备||Eyeshields,Gloves,type N95 (US),type P1 (EN143) respirator filter|
Copper-catalyzed intramolecular oxidative c?h functionalization and c?n formation of 2-aminobenzophenones: unusual pseudo-1,2-shift of the substituent on the aryl ring.
A good move: A copper-catalyzed intramolecular oxidative C?H functionalization of 2-aminobenzophenone affords two regioisomeric acridones. The reaction involves an unusual pseudo-1,2-migration of R(2)...Read More
An acridone-labeled DNA aptamer was synthesized to produce an aptamer probe. This aptamer probe could detect a specific molecule based on conformational changes upon binding of the specific molecules ...Read More
A novel series of 10-benzyl-9(10H)-acridinones were synthesized and evaluated as potent antileukemic activities. Structure-activity relationships are also studied....Read More
Structure-activity relationship studies of acridones as potential antipsoriatic agents. 1. Synthesis and antiproliferative activity of simple N-unsubstituted 10H-acridin-9-ones against human keratinocyte growth
A series of N-unsubstituted hydroxy-10H-acridin-9-ones were synthesized and evaluated for inhibitory action against HaCaT keratinocyte growth, in order to explore their potential as antipsoriatic agen...Read More
Structure-activity relationship studies of acridones as potential antipsoriatic agents. 2. Synthesis and antiproliferative activity of 10-substituted hydroxy-10H-acridin-9-ones against human keratinocyte growth
A series of 10-substituted hydroxy-10H-acridin-9-ones were synthesized and studied as potential antipsoriatic agents. The antiproliferative activity of the novel derivatives, which can be considered a...Read More
Extravascular transport of drugs in tumor tissue: effect of lipophilicity on diffusion of tirapazamine analogues in multicellular layer cultures.
The extravascular diffusion of antitumor agents is a key determinant of their therapeutic activity, but the relationships between physicochemical properties of drugs and their extravascular transport ...Read More
Cathepsins, also known as lysosomal cysteine peptidases, are members of the papain-like peptidase family, involved in different physiological processes. In addition, cathepsins are implicated in many ...Read More
The aim of the present study was to improve the cause-effect relationship between toxicant exposure and chironomid mouthpart deformities, by linking induction of mouthpart deformities to contaminated ...Read More
Minimalist probes for studying protein dynamics: thioamide quenching of selectively excitable fluorescent amino acids.
Fluorescent probe pairs that can be selectively excited in the presence of Trp and Tyr are of great utility in studying conformational changes in proteins. However, the size of these probe pairs can r...Read More
Extraction and chromatographic separation of the extracts of dried stem barks of Glycosmis macrantha lead to isolation of two new acridone alkaloids, macranthanine and 7-hydroxynoracronycine, and a kn...Read More
New tuftsin/retro-tuftsin conjugates were designed and synthesized using a classical fluorenylmethoxycarbonyl (Fmoc) solid phase procedure. All the peptide conjugates were divided into three series: 1...Read More
Visceral and cutaneous leishmaniases are an important public health problem in endemic geographic regions in 88 countries worldwide, with around 12 million infected people. Treatment options are limit...Read More
Acridones carrying an appropriate substituent at N-10 showed significant fluorescence changes on interacting with ATP in HEPES buffer at pH 7.2. The selectivity and sufficient binding of these probes ...Read More
Cathepsin V is a lysosomal cysteine peptidase highly expressed in thymus, testis and corneal epithelium. Eleven acridone alkaloids were isolated from Swinglea glutinosa (Bl.) Merr. (Rutaceae), with ei...Read More
Two new O-prenylated acridone alkaloids, balsacridone A (1) and B (2), together with eighteen known compounds were isolated from the methanol extract from the stems of Balsamocitrus paniculata, a Came...Read More
The acridone derivative MBLI-87 sensitizes breast cancer resistance protein-expressing xenografts to irinotecan
The breast cancer resistance protein ABCG2 confers cellular resistance to irinotecan (CPT-11) and its active metabolite SN-38. We utilised ABCG2-expressing xenografts as a model to evaluate the abilit...Read More
Presence and ex vivo formation of acridone in blood of patients routinely treated with carbamazepine: exploration of the 9-acridinecarboxaldehyde pathway.
Carbamazepine (CBZ) is a useful anticonvulsive drug associated with rare severe adverse drug reactions. The physio-pathological mechanisms of these reactions are unknown although evidence of immunolog...Read More
Development of highly predictive 3D-QSAR CoMSIA models for anthraquinone and acridone derivatives as telomerase inhibitors targeting G-quadruplex DNA telomere
G-quadruplex structures of DNA represent a potentially useful target for anticancer drugs. Telomerase enzyme, involved in immortalization of cancer cells is inhibited by stabilization of G-quadruplex ...Read More
Phytochemical analysis of different organs of the rutaceaeous plant Severinia buxifolia led to the isolation of a new limonoid, a new acridone alkaloid, and a new flavone. Structure elucidation and si...Read More
Design, synthesis and evaluation of 4,5-di-substituted acridone ligands with high G-quadruplex affinity and selectivity, together with low toxicity to normal cells
A series of 4,5-di-substituted acridones have been designed and synthesized. Several compounds show high affinity for telomeric G-quadruplex DNA in classical and competition FRET assays, together with...Read More
Design, synthesis and evaluations of acridone derivatives using Candida albicans-Search for MDR modulators led to the identification of an anti-candidiasis agent
In order to search for MDR modulators, rationally designed acridone derivatives were investigated for their effect on influx or efflux of Rhodamine6G (R6G) in CAI4 cells. Results of these investigatio...Read More
Inhibition of subgenomic hepatitis C virus RNA replication by acridone derivatives: identification of an NS3 helicase inhibitor.
We report the synthesis and structure-activity relationship (SAR) of a large series of acridones and acridone-fragment derivatives designed on the basis of the selective antihepatitis C virus (HCV) ac...Read More
Hybrid fluorescent conjugates of COX-2 inhibitors: search for a COX-2 isozyme imaging cancer biomarker.
The observation that the cyclooxygenase-2 (COX-2) isozyme is over-expressed in multiple types of cancer, relative to that in adjacent non-cancerous tissue, prompted this investigation to prepare a gro...Read More
Mechanism-based CYP2D6 inactivation by acridone alkaloids of Indonesian medicinal plant Lunasia amara.
Fourteen acridone alkaloids isolated from Lunasia amara Blanco were tested for their mechanism-based inhibition on human liver microsomal dextromethorphan O-demethylation activity, a prototype marker ...Read More
Cycloatalaphylline-A (1), N-methylcycloatalaphylline-A (2) and N-methyl-buxifoliadine-E (3), along with eight known acridone alkaloids and two known coumarins were isolated from the root of Atalantia ...Read More
Synthesis of novel heme-interacting acridone derivatives to prevent free heme-mediated protein oxidation and degradation.
Heme is an important prosthetic molecule for various hemoproteins and serves important function in living aerobic organisms. But degradation of hemoprotein, for example, hemoglobin during different pa...Read More