- HETEROCYCLIC COMPOUNDS AS INHIBITORS OF HPK1
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This disclosure relates to heterocyclics as inhibitors of HPK1, in particular relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising said compound that useful for treatment of HPK1 mediated diseases and conditions such as cancer. (I)
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Page/Page column 203
(2021/01/29)
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- A Suite of “Minimalist” Photo-Crosslinkers for Live-Cell Imaging and Chemical Proteomics: Case Study with BRD4 Inhibitors
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Affinity-based probes (AfBPs) provide a powerful tool for large-scale chemoproteomic studies of drug–target interactions. The development of high-quality probes capable of recapitulating genuine drug–target engagement, however, could be challenging. “Mini
- Pan, Sijun,Jang, Se-Young,Wang, Danyang,Liew, Si Si,Li, Zhengqiu,Lee, Jun-Seok,Yao, Shao Q.
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supporting information
p. 11816 - 11821
(2017/09/06)
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- Further studies on bis-charged tetraazacyclophanes as potent inhibitors of small conductance Ca2+-activated K+ channels
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Previously, quinolinium-based tetraazacyclophanes, such as UCL 1684 and UCL 1848, have been shown to be extraordinarily sensitive to changes in chemical structure (especially to the size of the cyclophane system) with respect to activity as potent non-peptidic blockers of the small conductance Ca 2+-activated K+ ion channels (SKCa). The present work has sought to optimize the structure of the linking chains in UCL 1848. We report the synthesis and SKCa channel-blocking activity of 29 analogues of UCL 1848 in which the central CH2 of UCL 1848 is replaced by other groups X or Y = O, S, CF2, CO, CHOH, CC, CHCH, CHMe to explore whether subtle changes in bond length or flexibility can improve potency still further. The possibility of improving potency by introducing ring substituents has also been explored by synthesizing and testing 25 analogues of UCL 1684 and UCL 1848 with substituents (NO2, NH2, CF 3, F, Cl, CH3, OCH3, OCF3, OH) in the 5, 6 or 7 positions of the aminoquinolinium rings. As in our earlier work, each compound was assayed for inhibition of the afterhyperpolarization (AHP) in rat sympathetic neurons, an action mediated by the SK3 subtype of the SK Ca channel. One of the new compounds (39, R7 = Cl, UCL 2053) is twice as potent as UCL 1848 and UCL 1684: seven are comparable in activity.
- Yang, Donglai,Arifhodzic, Lejla,Ganellin, C. Robin,Jenkinson, Donald H.
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supporting information
p. 907 - 923
(2013/07/27)
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- Inhibitors of the mevalonate pathway of streptococcus pneumoniae
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Compounds and related methods as can be used for selective mevalonate pathway inhibitors.
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Page/Page column 11
(2011/08/04)
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- Mevalonate analogues as substrates of enzymes in the isoprenoid biosynthetic pathway of Streptococcus pneumoniae
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Survival of the human pathogen Streptococcus pneumoniae requires a functional mevalonate pathway, which produces isopentenyl diphosphate, the essential building block of isoprenoids. Flux through this pathway appears to be regulated at the mevalonate kina
- Kudoh, Takashi,Park, Chan Sun,Lefurgy, Scott T.,Sun, Meihao,Michels, Theodore,Leyh, Thomas S.,Silverman, Richard B.
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experimental part
p. 1124 - 1134
(2010/04/26)
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- An approach towards the C1-C16 fragment of antineoplastic macrolide bryostatins by kinetic resolution of a racemic terminal epoxide using Jacobsen's catalyst
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A stereo- and enantioselective approach towards the C1-C16 fragment of bryostatins is reported using Jacobsen's catalyst for kinetic resolution of a terminal epoxide, a Horner-Wadsworth-Emmons coupling reaction and a 1,4-Michael type cyclization as key steps.
- Yadav,Bandyopadhyay,Kunwar
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p. 4907 - 4911
(2007/10/03)
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- Synthesis of a C1-C9 fragment of rhizoxin
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A C1-C9 fragment of the antitumour macrolide rhizoxin has been synthesised. An Evans' asymmetric aldol reaction was used to set up the first two chiral centres, and an α,β-unsaturated δ-lactone was then formed on the acyclic system by an intramolecular Wadsworth-Emmons reaction. Stereoselective hydrogenation was used to set up the cis relative stereochemistry in the saturated δ-lactone ring. (C) 2000 Published by Elsevier Science Ltd.
- Davenport,Regan
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p. 7619 - 7622
(2007/10/03)
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