- Discovery of DS68702229 as a potent, orally available NAMPT (Nicotinamide Phosphoribosyltransferase) Activator
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Nicotinamide phosphoribosyltransferase (NAMPT) catalyzes the rate-limiting step of the nicotinamide adenine dinucleotide (NAD+) salvage pathway. Because NAD+ plays a pivotal role in energy metabolism and boosting NAD+ has
- Akiu, Mayuko,Tsuji, Takashi,Iida, Kouki,Sogawa, Yoshitaka,Terayama, Koji,Yokoyama, Mika,Tanaka, Jun,Asano, Daigo,Honda, Tomohiro,Sakurai, Ken,Pinkerton, Anthony B.,Nakamura, Tsuyoshi
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p. 1110 - 1110
(2021/11/20)
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- Macrocyclic derivative of pyrazole[3,4-d]pyrimidin-3-one and pharmaceutical composition and application thereof
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The present invention relates to a macrocyclic derivative of pyrazole[3,4-d]pyrimidin-3-one as shown in the formula (I) and/or a pharmaceutically acceptable salt thereof, and a composition of a compound of the formula (I) and/or a pharmaceutically acceptable salt thereof, a preparation method thereof, application thereof as a Wee1 inhibitor and application thereof as a sensitizer for cancer chemotherapy or radiotherapy. The macrocyclic derivative of pyrazole[3,4-d]pyrimidin-3-one can effectively inhibit Wee1 and related signaling pathways, and has good cancer treatment and/or relieving effect.The formula is shown in the description.
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Paragraph 0332; 0558; 0559; 0560
(2018/10/19)
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- Total synthesis of the photoprotecting dipyrrolobenzoquinone (+)-terreusinone
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The first synthesis of (+)-terreusinone 1, a dipyrrolobenzoquinone with a potent UV-A protecting capability, is described. Key transformations include a one-pot Larock indolization-Sonogashira coupling reaction and the hydroamination of an unsubstituted o
- Wang, Christy,Sperry, Jonathan
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scheme or table
p. 6444 - 6447
(2012/02/05)
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- Synthesis of ring size seco-analogs of the antitumor antibiotic CC-1065 by two consecutive transition metal-initiated transformations
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Novel seco-analogs of CC-1065 1 were synthesized from comercially available nitroaniline by reduction, bromination, bisulfonation and bisallylation followed by reaction with tert-butyllithium, zirconocene and iodine. The obtained quinoline 6 was then transformed into 17 and 18, which, upon treatment with Pd0, led to 21 and 22, respectively. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003.
- Tietze, Lutz F.,Looft, Jan,Feuerstein, Tim
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p. 2749 - 2755
(2007/10/03)
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- RADIOLABELED FARNESYL-PROTEIN TRANSFERASE INHIBITORS
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The present invention is directed toward radiolabeled farnesyl-protein transferase inhibitor compounds which are useful to label FPTase in assays, whether cell-based, tissue-based or in whole animal. The tracers can also be used in competitive binding assays to obtain information on the interaction of unlabeled FTIs with FPTase.
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- Heteroaryl spiroethercycloalkyl tachykinin receptor antagonists
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The present invention is directed to certain novel compounds represented by structural formula I: STR1 or a pharmaceutically acceptable salt thereof, wherein R 3, R 6, R 7, R 8, R 11, R 12, R 13, A, m, n and the dashed lines are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.
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- Efficient synthesis of the pharmacophore of the highly potent antitumor antibiotic CC-1065
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The pharmacophore CPI (3) of the potent antitumor antibiotic CC-1065 (1) was synthesized in a very short reaction sequence of 11 steps with an overall yield of 23 %. The key steps are two consecutive cyclizations mediated by organotransition metal complexes, which form first the pyrroline and then the pyrrole ring in 3. Thus, halogen metal exchange of the N,N'-bisallylbromobenzene with tBuLi and subsequent reaction with Cp2ZrMeCl gave 11 as a single product in 60 % yield after quenching with two equivalents of iodine. Transformation of the iodomethyl group in 11 into an acetoxymethyl group, followed by Heck reaction, isomerization, and reductive cleavage, provided the pyrroloindoline system 4, which was converted into 3.
- Tietze, Lutz F.,Buhr, Wilm,Looft, Jan,Grote, Thomas
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p. 1554 - 1560
(2007/10/03)
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- POLYBROMINATED AROMATIC COMPOUNDS. III. SYNTHESIS OF BROMINE-SUBSTITUTED ANISOLES
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Reliable methods were developed for the synthesis of di-, tri-, and tetrabromoanisoles, and all the possible individual isomers were synthesized.The structures of the isomers were proved by alternative synthesis and spectral methods (PMR, IR).It was shown that the published data are incorrect in a number of cases; either the final product was assigned the incorrect structure, or the published methods led to mixture of the various isomers.
- Shishkin, V. N.,Tanaseichuk, B. S.,Lapin, K. K.,Ivkina, A. A.,Butin, K. P.
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p. 2357 - 2366
(2007/10/02)
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