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We synthesized 11 novel L-783277 derivatives, in which a structure rigidifying phenyl ring is incorporated into the 14-membered chiral resorcylic acid lactone system. The SAR study with these substances demonstrated that 17 possesses excellent kinase selectivity against a panel of 335 kinases in contrast to L-783277 and inhibits VEGFR3, VEGFR2 and FLT3 with single-digit nanomolar IC50 values. Also, we found that 21, a stereoisomer of 17, has excellent potency (IC50 = 9 nM) against VEGFR3 and selectivity over VEGFR2 and FLT3. 17, a potent dual VEGFR3 and VEGFR2 inhibitor, effectively suppresses both lymphangiogenesis and angiogenesis in a 3D-microfluidic tumor lymphangiogenesis assay and in vivo corneal assay while SAR131675 blocks only lymphangiogenesis. In addition, 17 blocks the endothelial tube formation and suppresses proliferation of PHE tumor vascular model. 17 will be a valuable template for developing therapeutically active and selective substances that target both lymphangiogenesis and angiogenesis.
This article was published in the following journal.
Name: Journal of medicinal chemistry
The intriguing structural complexity and bioactivities of the alkaloids have long attracted much attention. Herein, we report the first and enantioselective total synthesis of alkaloid dapholdhamine...
Chitosan as a biopolymer is an attractive vehicle for biomedical applications due to its unique characteristics. In order to improve chitosan's physicochemical features, chemical modification has been...
Carbonic acid was synthesized within an ice containing water and carbon dioxide by irradiation of ~9 eV photons. Vacuum UltraViolet (VUV)/UltraViolet (UV) photoabsorption spectra of the irradiated i...
Herein, we reported the total syntheses of traumatic lactone and rhizobialide via the strategy of utilizing allenoic acid to construct the lactone ring. The key starting materials, allenoic acids, cou...
This study evaluates the addition of Ginkgo Diterpene Lactone Meglumine Injection to aspirin in the treatment of acute ischemic stroke.Half of patient will receive Ginkgo Diterpene Lactone...
The aim of this study is to evaluate the safety and effectivity of Ginkgo diterpene lactone meglumine injection tn the treatment of acute ischemic stroke
The purpose of this study is to evaluate the satiating effects of a meat derivative and a satiating compound on overweight subjects (BMI ≥25 and
The purposes of this study include: - Determination of the change in clearance of topotecan and topotecan lactone between day 1 and day 14 for patients receiving treatment with p....
The purpose of the study is to determine the effect of enamel matrix protein derivative on an inflamed, periodontal-involved tooth. The hypothesis to be studied is that enamel matrix deriv...
Metabolite of ASCORBIC ACID and the oxidized form of the lactone DEHYDROASCORBIC ACID.
The reversibly oxidized form of ascorbic acid. It is the lactone of 2,3-DIKETOGULONIC ACID and has antiscorbutic activity in man on oral ingestion.
(S-(E))-3,4,5,6,8,10-Hexahydro-14,16-dihydroxy-3-methyl-1H-2-benzoxacyclotetradecin-1,7(8H)-dione. One of a group of compounds known under the general designation of resorcylic acid lactones. Cis, trans, dextro and levo forms have been isolated from the fungus Gibberella zeae (formerly Fusarium graminearum). They have estrogenic activity, cause toxicity in livestock as feed contaminant, and have been used as anabolic or estrogen substitutes.
An analytical method for detecting and measuring FLUORESCENCE in compounds or targets such as cells, proteins, or nucleotides, or targets previously labeled with FLUORESCENCE AGENTS.
A very strong halogenated derivative of acetic acid. It is used in acid catalyzed reactions, especially those where an ester is cleaved in peptide synthesis.
An assay is an analytic procedure for qualitatively assessing or quantitatively measuring the presence or amount or the functional activity of a target entity. This can be a drug or biochemical substance or a cell in an organism or organic sample. ...
Blood is a specialized bodily fluid that delivers necessary substances to the body's cells (in animals) – such as nutrients and oxygen – and transports waste products away from those same cells. In vertebrates, it is composed of blo...