- Auto-tandem PET and EnT photocatalysis by crude chlorophyll under visible light towards the oxidative functionalization of indoles
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Chlorophyll is the most abundant photocatalytic pigment that enables plants to absorb solar energy and convert it to energy storage molecules. Herein, we report a tandem photocatalytic approach utilizing the natural pigment chlorophyll in crude form to achieve photoinduced electron transfer (PET) and energy transfer (EnT) towards the oxidative functionalization of indoles. Redox potentials, ESR, fluorescence quenching and UV experiments have evidenced the dual catalytic activity of chlorophyll. The highlight of the study is the auto-tandem photocatalytic role of chlorophyll to enable the green oxidation of indoles using molecular oxygen as the oxidant, water as the reaction medium, and photochemical energy from the visible region of the spectrum.
- Banu, Saira,Choudhari, Shubham,Patel, Girija,Yadav, Prem P.
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supporting information
p. 3039 - 3047
(2021/05/05)
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- Thiazolidine derivatives or salts thereof as an active ingredient an inhibitor Pim
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PROBLEM TO BE SOLVED: To provide compounds which have excellent Pim inhibitory action and are useful as pharmaceuticals.SOLUTION: A compound is a thiazolidine derivative represented by the general formula (1) in the figure, or a salt thereof. (In the formula, X represents O or S; Rrepresents a hydrogen atom or a Calkyl group; Z, Z, Z, Z, Zand Zeach independently represent CH or N; Y represents an optionally substituted, divalent Caromatic hydrocarbon group or the like; Am represents a disubstituted amino group, or an optionally substituted, nitrogen-containing saturated heterocyclic group; and Rand Reach independently represent a hydrogen atom, a halogen atom, an alkyl group or the like.)
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Paragraph 0721; 0723
(2018/10/19)
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- Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR
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The identification and lead optimization of a series of pyridopyrimidinone derivatives are described as a novel class of efficacious dual PI3K/mTOR inhibitors, resulting in the discovery of 31. Compound 31 exhibited high enzyme activity against PI3K and mTOR, potent suppression of Akt and p70s6k phosphorylation in cell assays, and good pharmacokinetic profile. Furthermore, compound 31 demonstrated in vivo efficacy in a PC-3M tumor xenograft model.
- Yu, Tao,Li, Ning,Wu, Chengde,Guan, Amy,Li, Yi,Peng, Zhengang,He, Miao,Li, Jie,Gong, Zhen,Huang, Lei,Gao, Bo,Hao, Dongling,Sun, Jikui,Pan, Yan,Shen, Liang,Chan, Chichung,Lu, Xiulian,Yuan, Hongyu,Li, Yongguo,Li, Jian,Chen, Shuhui
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supporting information
p. 256 - 261
(2018/03/21)
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- Intermolecular Aryl C?H Amination through Sequential Iron and Copper Catalysis
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A mild, efficient and regioselective method for para-amination of activated arenes has been developed through a combination of iron and copper catalysis. A diverse range of products were obtained from an operationally simple one-pot, two-step procedure involving bromination of the aryl substrate with the powerful Lewis acid iron(III) triflimide, followed by a copper(I)-catalysed N-arylation reaction. This two-step dehydrogenative process for the regioselective coupling of aromatic C?H bonds with non-activated amines was applicable to anisole-, phenol-, aniline- and acetanilide-type aryl compounds. Importantly, the arene substrates were used as the limiting reagent and required no protecting-group manipulations during the transformation.
- Mostafa, Mohamed A. B.,Calder, Ewen D. D.,Racys, Daugirdas T.,Sutherland, Andrew
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supporting information
p. 1044 - 1047
(2017/02/05)
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- Discovery of a novel series of thienopyrimidine as highly potent and selective PI3K inhibitors
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Inhibition of the phosphoinositide 3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling pathway provides a promising new approach for cancer therapy. Through a rational design, a novel series of thienopyrimidine was discovered as highly pote
- Han, Fangbin,Lin, Songwen,Liu, Peng,Liu, Xiujie,Tao, Jing,Deng, Xiaobing,Yi, Chongqin,Xu, Heng
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supporting information
p. 434 - 438
(2015/04/27)
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- FUSED HETEROARYLS AND THEIR USES
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Provided are certain fused heteroaryls, compositions thereof and methods of use therefor.
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Paragraph 0233; 0235
(2013/07/31)
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- FUSED HETEROARYLS AND THEIR USES
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Provided are certain fused heteroaryls, compositions thereof and methods of use therefor.
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Page/Page column 82
(2012/04/04)
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- Identification of 4,5-dihydro-1 H -pyrazolo[4,3- h ]quinazoline Derivatives as a new class of orally and selective polo-like kinase 1 inhibitors
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Polo-like kinase 1 (Plk1) is a fundamental regulator of mitotic progression whose overexpression is often associated with oncogenesis and therefore is recognized as an attractive therapeutic target in the treatment of proliferative diseases. Here we discuss the Structure-activity relationship of the 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline class of compounds that emerged from a high throughput screening (HTS) campaign as potent inhibitors of Plk1 kinase. Furthermore, we describe the discovery of 49, 8-{[2-methoxy-5-(4- methylpiperazin-1-yl)phenyl]amino}-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h] quinazoline-3-carboxamide, as a highly potent and specific ATP mimetic inhibitor of Plk1 (IC50 = 0.007 μM) as well as its crystal structure in complex with the methylated Plk136-345 construct. Compound 49 was active in cell proliferation against different tumor cell lines with IC 50 values in the submicromolar range and active in vivo in the HCT116 xenograft model where it showed 82% tumor growth inhibition after repeated oral administration.
- Beria, Italo,Ballinari, Dario,Bertrand, Jay Aaron,Borghi, Daniela,Bossi, Roberto Tiberio,Brasca, Maria Gabriella,Cappella, Paolo,Caruso, Michele,Ceccarelli, Walter,Ciavolella, Antonella,Cristiani, Cinzia,Croci, Valter,De Ponti, Anna,Fachin, Gabriele,Ferguson, Ronald Dale,Lansen, Jacqueline,Moll, Jurgen Karl,Pesenti, Enrico,Posteri, Helena,Perego, Rita,Rocchetti, Maurizio,Storici, Paola,Volpi, Daniele,Valsasina, Barbara
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experimental part
p. 3532 - 3551
(2010/09/11)
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- SUBSTITUTED PYRAZOLO-QUINAZOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
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Pyrazolo-quinazoline derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may
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Page/Page column 87; 88
(2008/12/06)
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- Oxidative cleavage reaction of substituted indoles catalyzed by plant cell cultures
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We have developed a novel method for the oxidative cleavage of indole carbon double bonds in the presence of H2O2 using plant cell cultures as peroxidase. The oxidative method has some advantage, as features such as mild reactions, good yields, easy work-up and safety.
- Takemoto, Masumi,Iwakiri, Yasutaka,Tanaka, Kiyoshi
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p. 373 - 383
(2008/03/12)
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- Synthesis and SAR of indazole-pyridine based protein kinase B/Akt inhibitors
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A series of heteroaryl-pyridine containing inhibitors of Akt are reported. The synthesis and structure-activity relationships are discussed, leading to the discovery of a indazole-pyridine analogue (Ki = 0.16 nM). These compounds bind in the ATP binding site, are potent, ATP competitive, and reversible inhibitors of Akt activity. No selectivity amongst the Akt isoforms is observed for this analogue, but there is good selectivity against an panel of other kinases. It is least selective for other members of the AGC family of kinases but is nonetheless 40-fold selective for Akt over PKA. The compound shows cellular activity and significantly slows tumor growth in vivo.
- Woods, Keith W.,Fischer, John P.,Claiborne, Akiyo,Li, Tongmei,Thomas, Sheela A.,Zhu, Gui-Dong,Diebold, Robert B.,Liu, Xuesong,Shi, Yan,Klinghofer, Vered,Han, Edward K.,Guan, Ran,Magnone, Shayna R.,Johnson, Eric F.,Bouska, Jennifer J.,Olson, Amanda M.,Jong, Ron de,Oltersdorf, Tilman,Luo, Yan,Rosenberg, Saul H.,Giranda, Vincent L.,Li, Qun
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p. 6832 - 6846
(2007/10/03)
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- Kinase inhibitors
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Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
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- Kinase inhibitors
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Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
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Page/Page column 27
(2010/01/31)
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