247174-18-1Relevant articles and documents
Mononuclear Zn(ii)- and Cu(ii)-complexes of a hydroxynaphthalene-derived dipicolylamine: Fluorescent sensing behaviours toward pyrophosphate ions
Roy, Basab,Rao, Alla Sreenivasa,Ahn, Kyo Han
, p. 7774 - 7779 (2011)
Mononuclear Zn(ii)-DPA and Cu(ii)-DPA complexes crafted on 2-hydroxy-6-cyanonaphthalene fluorophore selectively recognize PPi over ATP and other anions including inorganic phosphates in aqueous medium, showing turn-on type fluorescence enhancements. Coordination of a hydroxyl group of the fluorophore, directly or in alkoxy form, to the central metal ion is crucial for the sensing processes. Both the complexes elicit a fluorescence increase in a time-dependent fashion.
SMALL MOLECULE INHIBITORS OF A PROTEIN COMPLEX
-
Paragraph 00180; 00181, (2020/12/29)
Compositions and methods for treating thrombosis, inflammation, and atherosclerosis by administration of a compound that binds to KRIT1 to inhibit binding with HEG1.
Discovery and Rational Design of Natural-Product-Derived 2-Phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine Analogs as Novel and Potent Dipeptidyl Peptidase 4 (DPP-4) Inhibitors for the Treatment of Type 2 Diabetes
Li, Shiliang,Xu, Hongling,Cui, Shichao,Wu, Fangshu,Zhang, Youli,Su, Mingbo,Gong, Yinghui,Qiu, Shaobing,Jiao, Qian,Qin, Chun,Shan, Jiwei,Zhang, Ming,Wang, Jiawei,Yin, Qiao,Xu, Minghao,Liu, Xiaofeng,Wang, Rui,Zhu, Lili,Li, Jia,Xu, Yufang,Jiang, Hualiang,Zhao, Zhenjiang,Li, Jingya,Li, Honglin
, p. 6772 - 6790 (2016/08/05)
Starting from the lead isodaphnetin, a natural product inhibitor of DPP-4 discovered through a target fishing docking based approach, a series of novel 2-phenyl-3,4-dihydro-2H-benzo[f]chromen-3-amine derivatives as potent DPP-4 inhibitors are rationally designed utilizing highly efficient 3D molecular similarity based scaffold hopping as well as electrostatic complementary methods. Those ingenious drug design strategies bring us approximate 7400-fold boost in potency. Compounds 22a and 24a are the most potent ones (IC50 ≈ 2.0 nM) with good pharmacokinetic profiles. Compound 22a demonstrated stable pharmacological effect. A 3 mg/kg oral dose provided >80% inhibition of DPP-4 activity within 24 h, which is comparable to the performance of the long-acting control omarigliptin. Moreover, the efficacy of 22a in improving the glucose tolerance is also comparable with omarigliptin. In this study, not only promising DPP-4 inhibitors as long acting antidiabetic that are clinically on demand are identified, but the target fish docking and medicinal chemistry strategies were successfully implemented.
Benzo-hexatomic ring derivative used as DPP-4 inhibitor and application of benzo-hexatomic ring derivative
-
Paragraph 0345; 0346; 0347; 0348, (2016/10/09)
The invention relates to a benzo-hexatomic ring derivative used as a DPP-4 inhibitor and application of the benzo-hexatomic ring derivative, in particular to compounds shown as in formula I, medicine compositions with the compounds shown as in the formula I and application of the compounds in preparing medicines for treating diseases related to DPP-4 or inhibiting the DPP-4.
Decarbonylative halogenation by a vanadium complex
Rana, Sujoy,Haque, Rameezul,Santosh, Ganji,Maiti, Debabrata
, p. 2927 - 2932 (2013/04/24)
Metal-catalyzed halogenation of the C-H bond and decarbonylation of aldehyde are conventionally done in nature. However, metal-mediated decarbonylative halogenation is unknown. We have developed the first metal-mediated decarbonylative halogenation reaction starting from the divanadium oxoperoxo complex K3V5+2(O 22-)4(O2-)2(μ-OH) (1). A concerted decarbonylative halogenation reaction was proposed based on experimental observations.
Synthesis and cytotoxic activity of benzo[a]acronycine and benzo[b]acronycine substituted on the A ring
Gaslonde, Thomas,Covello, Fabiola,Velazquez-Alonso, Laura,Léonce, Stéphane,Pierré, Alain,Pfeiffer, Bruno,Michel, Sylvie,Tillequin, Franois
experimental part, p. 1861 - 1873 (2011/05/07)
The impact of substitutions at position 10 in the A ring of the cytotoxic benzo[a]acronycine and benzo[b]acronycine series has been explored. 10-Bromobenzo[a] and 10-bromobenzo[b]acronycine were prepared in 12% and 15% yield respectively from commercially
17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS FOR THE TREATMENT OF HORMONE-RELATED DISEASES
-
Page/Page column 14-15, (2010/08/18)
The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases.The invention further relates to suitable inhibitors and to a method for the production thereof.
Synthesis, biological evaluation and molecular modelling studies of novel ACD- and ABD-ring steroidomimetics as inhibitors of CYP17
Pinto-Bazurco Mendieta, Mariano A.E.,Negri, Matthias,Jagusch, Carsten,Hille, Ulrike E.,Mueller-Vieira, Ursula,Schmidt, Dirk,Hansen, Klaus,Hartmann, Rolf W.
, p. 267 - 273 (2008/09/17)
Two novel classes of non-steroidal substrate mimetics were synthesised and examined for their potency as inhibitors of human CYP17. Selected compounds were tested for inhibition of hepatic CYP enzymes 3A4, 1A2, 2C9 and 2C19. The most promising compound 15
Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1): Design, synthesis, biological evaluation, and pharmacokinetics
Marchais-Oberwinkler, Sandrine,Krachten, Patricia,Frotscher, Martin,Ziegler, Erika,Neugebauer, Alexander,Bhoga, Umadevi,Bey, Emmanuel,Müller-Vieira, Ursula,Messinger, Josef,Thole, Hubert,Hartmann, Rolf W.
supporting information; experimental part, p. 4685 - 4698 (2009/07/19)
17β-Estradiol (E2) is implicated in the genesis and the development of estrogen-dependent diseases. Its concentration is mainly regulated by 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1), which catalyzes the reduction of the weak estrogen estrone (E1) to the highly potent E2. This enzyme is thus an important target for the treatment of hormone-dependent diseases. Thirty-seven novel substituted 6-phenyl-2-naphthols were synthesized and evaluated for 17β-HSD1 inhibition, selectivity toward 17β-HSD2 and the estrogen receptors (ERs) α and β, and pharmacokinetic properties. SAR studies revealed that the compounds most likely bind according to binding mode B to the active site, i.e., the 6-phenyl moiety mimicking the steroidal A-ring. While substitution at the phenyl ring decreased activity, introduction of substituents at the naphthol moiety led to highly active compounds, especially in position 1. The 1-phenyl compound 32 showed a very high inhibitory activity for 17β-HSD1 (IC50 = 20 nM) and good selectivity (17β-HSD2 and ERs) and pharmacokinetic properties after peroral application.
C17,20-lyase inhibitors. Part 2: Design, synthesis and structure-activity relationships of (2-naphthylmethyl)-1H-imidazoles as novel C17,20-lyase inhibitors
Matsunaga, Nobuyuki,Kaku, Tomohiro,Ojida, Akio,Tanaka, Toshimasa,Hara, Takahito,Yamaoka, Masuo,Kusaka, Masami,Tasaka, Akihiro
, p. 4313 - 4336 (2007/10/03)
A series of 1- and 4-(2-naphthylmethyl)-1H-imidazoles (3 and 4) has been synthesized and evaluated as C17,20-lyase inhibitors. Several 6-methoxynaphthyl derivatives showed potent C17,20-lyase inhibition, suppression of testosterone biosynthesis in rats and reduction in the weight of prostate and seminal vesicles in rats, whereas most of these compounds increased the liver weight after consecutive administrations. The effect on the liver weight was removed by incorporation of a hydroxy group and an isopropyl group at the methylene bridge, as seen in (S)-28d and (S)-42. Selectivity for C 17,20-lyase over 11β-hydroxylase is also discussed, and (S)-42 was found to be a more than 260-fold selective inhibitor. Furthermore, (S)-42 showed a potent suppression of testosterone biosynthesis after a single oral administration in monkeys. These data suggest that (S)-42 may be a promising agent for the treatment of androgen-dependent prostate cancer.