151071-03-3Relevant articles and documents
Potent and Highly Selective Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors Act as Chemotherapeutic Potentiators in Acute Myeloid Leukemia and T-Cell Acute Lymphoblastic Leukemia
Verma, Kshitij,Zang, Tianzhu,Penning, Trevor M.,Trippier, Paul C.
supporting information, p. 3590 - 3616 (2019/04/26)
Aldo-keto reductase 1C3 (AKR1C3) catalyzes the synthesis of 9α,11β-prostaglandin (PG) F2α and PGF2α prostanoids that sustain the growth of myeloid precursors in the bone marrow. The enzyme is overexpressed in acute myeloid leukemia (
HIGHLY SELECTIVE AKR1C3 INHIBITORS AND METHODS OF USE THEREOF
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Page/Page column 63, (2018/09/08)
The present invention includes methods and compositions that inhibit AKR1C3 enzymatic activity and consequently reduces androgen receptor (AR) transactivation, AR and prostate specific antigen (PSA) expression levels in, for example, prostate cancer, cast
Ph3PAuNTf2 as a superior catalyst for the selective synthesis of 2H-chromenes: Application to the concise synthesis of benzopyran natural products
Lykakis, Ioannis N.,Efe, Christina,Gryparis, Charis,Stratakis, Manolis
experimental part, p. 2334 - 2338 (2011/06/20)
Ph3PAuNTf2 (≈1 mol-%) catalyzes the selective cycloisomerization of substituted aryl propargyl ethers into 2H-chromenes in excellent yields. Benzofuran byproducts are formed only in the case of electron-deficient arenes, in up to 7% relative yield. The Ph 3PAuNTf2-catalyzed cyclization of aryl propargyl ethers was applied as a key step to the concise synthesis of the naturally occurring benzopyrans seselin, xanthyletin, precocenes I and II, 8-(3′,3′- dimethylallyl)wenteria chromene, and 2,2-dimethyl-8-prenylchromene-6-propenoic acid. Ph3PAuNTf2 is a general, highly efficient, and product-selective catalyst for the clean synthesis of 2H-chromenes from the cycloisomerization of aryl propargyl ethers.The Ph3PAuNTf 2-catalyzed cyclization was applied as a key step in the synthesis of several benzopyran-bearing naturally occurring substances. Copyright
Artepillin C isoprenomics: Design and synthesis of artepillin C isoprene analogues as lipid peroxidation inhibitor having low mitochondrial toxicity
Uto, Yoshihiro,Ae, Shutaro,Koyama, Daisuke,Sakakibara, Mitsutoshi,Otomo, Naoki,Otsuki, Mamoru,Nagasawa, Hideko,Kirk, Kenneth L.,Hori, Hitoshi
, p. 5721 - 5728 (2007/10/03)
We designed and synthesized isoprene analogues of artepillin C, a major component of Brazilian propolis, and investigated the inhibitory activity on lipid peroxidation of rat liver mitochondria (RLM) and RLM toxicity based on isoprenomics. We succeeded in
First total synthesis of artepillin C established by o,o′-diprenylation of p-halophenols in water
Uto, Yoshihiro,Hirata, Akihiko,Fujita, Tomoya,Takubo, Syunsuke,Nagasawa, Hideko,Hori, Hitoshi
, p. 2355 - 2357 (2007/10/03)
We have demonstrated that prenylation of phalophenols was dependent on the solvent effect and succeeded in o,o′-diprenylation of p-halophenols in water. Following the Mizoroki-Heck coupling of the diprenyl-piodophenol 3c with methyl acrylate and then hydr
Synthesis of Phenolic Natural Products Using Palladium Catalyzed Coupling Reactions
Bates, Roderick W.,Gabel, Christine J.,Ji, Jianhua,Rama-Devi, Thota
, p. 8199 - 8212 (2007/10/02)
Derivatives of 2,4-diiodophenol are shown to undergo palladium catalyzed carbonylation and alkyne coupling reactions in excellent to moderate yield and high regioselectivity.The scope of these reactions is explored.Palladium catalyzed reactions are employ
The synthesis of Plicatin B via the Heck reaction
Bates,Gabel
, p. 3547 - 3550 (2007/10/02)
The anti-microbial natural product Plicatin B has been synthesized in 53% overall yield using a Heck reaction as the key step. The optimum conditions for this reaction have been determined. Halophenols proved much less reactive than their corresponding ac
