- Synthesis of Small-Molecule Fluorescent Probes for the In Vitro Imaging of Calcium-Activated Potassium Channel KCa3.1
-
Small-molecule probes for the in vitro imaging of KCa3.1 channel-expressing cells were developed. Senicapoc, showing high affinity and selectivity for the KCa3.1 channels, was chosen as the targeting component. BODIPY dyes 15–20 were
- Br?mmel, Kathrin,Koch, Oliver,Konken, Christian Paul,Maisuls, Ivan,Maskri, Sarah,Peth?, Zoltan,Rieke, Marius,Schwab, Albrecht,Strassert, Cristian A.,Wünsch, Bernhard
-
-
Read Online
- First Total Synthesis and Investigation of the X-ray Crystal Structure of the Pyrano[3,2- a ]carbazole Alkaloid Clausenalansine A
-
We describe the first total synthesis of the recently discovered pyrano[3,2- a ]carbazole alkaloid clausenalansine A. The synthetic strategy for the construction of this formylpyrano[3,2- a ]carbazole is based on a sequence of Buchwald-Hartwig coupling, palladium(II)-catalyzed oxidative cyclization, Lewis acid promoted annulation of the pyran ring, and chemoselective oxidation of a methyl to a formyl group.
- L?sle, Valerie,Kataeva, Olga,Kn?lker, Hans-Joachim
-
-
Read Online
- Acylative desymmetrization of cyclic meso-1,3-diols by chiral DMAP derivatives
-
An efficient enantioselective acylative desymmetrization of cyclic meso-1,3-diols was developed by using a chiral DMAP derivative 1e having a 1,1¤-binaphthyl unit. The reactions required only 0.5mol% of the catalyst and showed good to excellent enantioselectivity. With this transformation, 5a, a key building block for the synthesis of natural products, was easily obtained in almost enantiomerically pure form after a single recrystallization. Control experiments revealed that tert-alcohol units on the catalyst were responsible for both the catalytic activity and enantioselectivity.
- Mandai, Hiroki,Hironaka, Tsubasa,Mitsudo, Koichi,Suga, Seiji
-
supporting information
p. 471 - 474
(2021/03/15)
-
- A Cationic Micelle as In Vivo Catalyst for Tumor-Localized Cleavage Chemistry
-
The emerging strategies of accelerating the cleavage reaction in tumors through locally enriching the reactants is promising. Yet, the applications are limited due to the lack of the tumor-selectivity for most of the reactants. Here we explored an alternative approach to leverage the rate constant by locally inducing an in vivo catalyst. We found that the desilylation-induced cleavage chemistry could be catalyzed in vivo by cationic micelles, and accelerated over 1400-fold under physiological condition. This micelle-catalyzed controlled release platform is demonstrated by the release of a 6-hydroxyl-quinoline-2-benzothiazole derivative (HQB) in two cancer cell lines and a NIR dye in mouse tumor xenografts. Through intravenous injection of a pH-sensitive polymer micelles, we successfully applied this strategy to a prodrug activation of hydroxyl camptothecin (OH-CPT) in tumors. Its “decaging” efficiency is 42-fold to that without cationic micelles-mediated catalysis. This micelle-catalyzed desilylation strategy unveils the potential that micelle may act beyond a carrier but a catalyst for local perturbing or activation.
- Chen, Mengqi,Ding, Zexuan,Hong, Hanyu,Li, Zi-Chen,Liu, Zhibo,Qi, Jianyuan,Rui, Yuchen,Wang, Chunhong
-
supporting information
p. 19750 - 19758
(2021/07/12)
-
- Phase-Transfer Catalyzed O-Silyl Ether Deprotection Mediated by a Cyclopropenium Cation
-
The use of a cyclopropenium cation as a phase-transfer catalyst for O-silyl ether deprotection is reported. Mechanistic insight into this deprotection methodology derived by linear free-energy relationships (LFER), quantum theory of atoms in molecules (QTAIM), and density functional theory (DFT) calculations are also provided.
- Mir, Roya,Dudding, Travis
-
p. 709 - 714
(2017/04/26)
-
- Synthesis of the Pyrano[3,2- a ]carbazole Alkaloids Koenine, Koenimbine, Koenigine, Koenigicine, and Structural Reassignment of Mukonicine
-
Using the palladium(II)-catalyzed oxidative cyclization of a diarylamine and the annulation of a dimethylpyran ring by Lewis acid promoted reaction with prenal as key steps, the total syntheses of the 6-oxygenated pyrano[3,2-a]carbazole alkaloids koenine and koenimbine, and of the 6,7-dioxygenated pyrano[3,2-a]carbazole alkaloids koenigine and koenigicine (koenimbidine, koenidine) were achieved. Moreover, these studies led to an improved synthetic route to the 2,6-dioxygenated carbazole alkaloid glycozolidol. Mukonicine, originally published as 6,8-dimethoxypyrano[3,2-a]carbazole, was found to be identical with koenigicine.
- Schuster, Christian,R?nnefahrt, Marika,Julich-Gruner, Konstanze K.,J?ger, Anne,Schmidt, Arndt W.,Kn?lker, Hans-Joachim
-
p. 150 - 160
(2015/12/26)
-
- Biphenyl compounds and their use as oestrogenic agents
-
Compounds of formula (I), wherein [X] represents aromatic carbocyclic rings (A) and (B), where R1, R2, R3, R4, R5, R6and R7are as defined in the description, salts thereof, a method and intermediates for preparing same, the use thereof as drugs, and pharmaceutical compositions containing same, are disclosed.
- -
-
Page column 8
(2010/11/29)
-
- Biphenyl compounds and use thereof as oestrogenic agents
-
A compound having the formula wherein R5 is an [A]—CH3, —[A]—C(OH)ZZ′ or —[A]—C(O)Z″ grouping where —[A]— is an alkylene, alkenylene or alkynylene radical or a single bond, and Z, Z′ and Z″ are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl radical; and R1, R2, R3, R4, R6, R7 and R8 are as defined in the description; the use thereof as a drug, pharmaceutical compositions containing same, a preparation method therefor, and intermediates of said method, are disclosed.
- -
-
-
- Biphenyl compounds and use thereof as oestrogenic agents
-
PCT No. PCT/FR97/00184 Sec. 371 Date Aug. 28, 1998 Sec. 102(e) Date Sep. 28, 1998 PCT Filed Jan. 30, 1997 PCT Pub. No. WO97/28116 PCT Pub. Date Aug. 7, 1997Compounds of formula (I), wherein [X] represents aromatic carbocyclic rings (A) and (B), where R1, R2, R3, R4, R5, R6 and R7 are as defined in the description, salts thereof, a method and intermediates for preparing same, the use thereof as drugs, and pharmaceutical compositions containing same, are disclosed.
- -
-
-
- Designing banana-shaped liquid crystals without Schiff's base units: m- Terphenyls, 2,6-diphenylpyridines and V-shaped tolane derivatives
-
This paper reports attempts to obtain (anti)ferroelectric switchable achiral banana-shaped molecules without Schiff's base units. For this purpose we have synthesized novel V-shaped molecules consisting of rigid angular central units [1,3-disubstituted be
- Shen, Dong,Diele, Siegmar,Pelzl, Gerhard,Wirth, Ina,Tschierske, Carsten
-
p. 661 - 672
(2007/10/03)
-
- Biphenyl compounds
-
Novel compounds of the formula STR1 wherein the substituents are defined as in the application and their salts with non-toxic, pharmaceutically acceptable acids and bases having 5-α-reductase inhibiting activity and a process and intermediates for their preparation.
- -
-
-
- 3-Chloropyridines, and their use in liquid-crystal mixtures
-
3-Chloropyridines, process for their preparation, and their use in liquid-crystal mixtures A 3-chloropyridine of the formula (I) STR1 in which the symbols have the following meaning: R1 and R2, independently of one another, are, for example, H or straight-chain or branched alkyl, A1, A2, A3 and A4 are identical or different and are, for example, 1,4-phenylene, pyrazine-2,5-diyl or trans-1,4-cyclohexylene, M1, M2, M3 and M4 are identical or different and are, for example, --O-- or --CO--O--, R3, R4, R6 and R7, independently of one another are, for example, H or straight-chain or branched alkyl, M5 is, for example, --O--CO-- or a single bond, k, l, m, n, o, p, q and r are zero or one, with the proviso that the sum k+m+p+r is less than 4 and greater than zero, can advantageously be employed as a component in ferroelectric liquid-crystal mixtures.
- -
-
-
- 3-fluoropyridines, process for their preparation, and their use in liquid-crystal mixtures
-
A 3-fluoropyridine of the formula (I) STR1 in which the symbols have the following meanings: R1 and R2, independently of one another, are, for example, H or straight-chain or branched alkyl, A1, A2, A3 and A4 are identical or different and are, for example, 1,4-phenylene, pyrazine-2,5-diyl or trans-1,4-cyclohexylene, M1, M2, M3 and M4 are identical or different and are, for example, --O-- or --CO--O--, R3, R4, R6 and R7, independently of one another are, for example, H or straight-chain or branched alkyl, M5 is for example, --O--CO-- or a single bond, k, l, m, n, o, p, q and r are zero or one, with the proviso that the sum k+m+p+r is less than 4 and greater than zero, can advantageously be employed as a component in ferroelectric liquid-crystal mixtures.
- -
-
-
- Quinoline ether alkanoic acids
-
Compounds having the formula: STR1 are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
- -
-
-