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79099-07-3Relevant articles and documents
Synthesis of (R)-(+)-1,2,3,6-Tetrahydro-4-[U-14C]phenyl-1-[(3-phenyl-3-cyclohexenyl-1 -yl)methyl]pyridine, a potential antipsychotic agent
Ekhato,Huang
, p. 57 - 63 (1995)
1,2,3,6-Tetrahydro-4-[U-14C]phenylpyridine (12) was synthesized and coupled to (R)-3-phenyl-3-cyclohexene-1-carboxylic acid to make the titled compound 7 in 21% overall yield. Purification considerations were an important factor in the choice of a reaction sequence to 7, and successful synthesis was facilitated by the superiority of BF3.OEt2 as dehydrating reagent in this system. This otherwise problematic sequence offers an efficient and simple route to compound 7 (PD 143188).
A Convenient Synthesis and Biological Research of Novel 5,6,7,8-Tetrahydro-1,6-naphthyridin-2(1H)-one Derivatives Hydrochloride as Cytotoxic Agents
Xu, Guiqing,Gao, Yuan,Sun, Bin,Peng, Lizeng,Mao, Longfei,Jiang, Yuqin,Ding, Qingjie
, p. 2151 - 2156 (2018)
A series of 5,6,7,8-tetrahydro-1,6-naphthyridin-2(1H)-one derivatives hydrochloride were obtained using a convenient and mild method from 4-piperidone monohydrate hydrochloride. The newly synthesized compounds and their derivatives were characterized by 1H NMR, 13C NMR, and high-resolution mass spectrometry. Furthermore, cytotoxicity in vitro of the synthesized compounds were screened using MTT or CCK8 assay. The results showed that some of the compounds showed potential antitumor activity. Among of them, compound 10a had effects against tumor cells (MOLM-13), and the half maximal inhibitory concentration value was 76?μmol/L.
FENTANYL HAPTENS FOR THE PREPARATION OF A FENTANYL VACCINE
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Paragraph 0195, (2021/07/24)
Described is the preparation of novel fentanyl haptens of Formula (1) through (6) and their use in the preparation of effective fentanyl vaccines.
ANTI-CD25 ANTIBODY-MAYTANSINE CONJUGATES AND METHODS OF USE THEREOF
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Paragraph 00402-00405, (2021/04/10)
The present disclosure provides anti-CD25 antibody-maytansine conjugate structures. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same.
ANTI-CD37 ANTIBODY-MAYTANSINE CONJUGATES AND METHODS OF USE THEREOF
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Paragraph 00409-00412, (2021/05/07)
The present disclosure provides anti-CD37 antibody-maytansine conjugate structures. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same.
Cobalt-Catalyzed Aerobic Oxidative Cleavage of Alkyl Aldehydes: Synthesis of Ketones, Esters, Amides, and α-Ketoamides
Li, Tingting,Hammond, Gerald B.,Xu, Bo
supporting information, p. 9737 - 9741 (2021/05/31)
A widely applicable approach was developed to synthesize ketones, esters, amides via the oxidative C?C bond cleavage of readily available alkyl aldehydes. Green and abundant molecular oxygen (O2) was used as the oxidant, and base metals (cobalt and copper) were used as the catalysts. This strategy can be extended to the one-pot synthesis of ketones from primary alcohols and α-ketoamides from aldehydes.
A general N-alkylation platform via copper metallaphotoredox and silyl radical activation of alkyl halides
Cabré, Albert,Dow, Nathan W.,MacMillan, David W. C.
supporting information, p. 1827 - 1842 (2021/07/07)
The catalytic union of amides, sulfonamides, anilines, imines, or N-heterocycles with a broad spectrum of electronically and sterically diverse alkyl bromides has been achieved via a visible-light-induced metallaphotoredox platform. The use of a halogen abstraction-radical capture (HARC) mechanism allows for room temperature coupling of C(sp3)-bromides using simple Cu(II) salts, effectively bypassing the prohibitively high barriers typically associated with thermally induced SN2 or SN1 N-alkylation. This regio- and chemoselective protocol is compatible with >10 classes of medicinally relevant N-nucleophiles, including established pharmaceutical agents, in addition to structurally diverse primary, secondary, and tertiary alkyl bromides. Furthermore, the capacity of HARC methodologies to engage conventionally inert coupling partners is highlighted via the union of N-nucleophiles with cyclopropyl bromides and unactivated alkyl chlorides, substrates that are incompatible with nucleophilic substitution pathways. Preliminary mechanistic experiments validate the dual catalytic, open-shell nature of this platform, which enables reactivity previously unattainable in traditional halide-based N-alkylation systems.
Pyrazolyl-pyrimidones inhibit the function of human solute carrier protein SLC11A2 (hDMT1) by metal chelation
Embaby, Ahmed,Hediger, Matthias A.,Javor, Sacha,Manatschal, Cristina,Poirier, Marion,Reymond, Jean-Louis,Bühlmann, Sven,Pujol-Giménez, Jonai
supporting information, p. 1023 - 1031 (2020/10/06)
Solute carrier proteins (SLCs) control fluxes of ions and molecules across biological membranes and represent an emerging class of drug targets. SLC11A2 (hDMT1) mediates intestinal iron uptake and its inhibition might be used to treat iron overload diseases such as hereditary hemochromatosis. Here we report a micromolar (IC50 = 1.1 μM) pyrazolyl-pyrimidone inhibitor of radiolabeled iron uptake in hDMT1 overexpressing HEK293 cells acting by a non-competitive mechanism, which however does not affect the electrophysiological properties of the transporter. Isothermal titration calorimetry, competition with calcein, induced precipitation of radioactive iron and cross inhibition of the unrelated iron transporter SLC39A8 (hZIP8) indicate that inhibition is mediated by metal chelation. Mapping the chemical space of thousands of pyrazolo-pyrimidones and similar 2,2′-diazabiaryls in ChEMBL suggests that their reported activities might partly reflect metal chelation. Such metal chelating groups are not listed in pan-assay interference compounds (PAINS) but should be checked when addressing SLCs.
C10-ALKYLENE SUBSTITUTED 13-MEMBERED MACROLIDES AND USES THEREOF
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Paragraph 00298, (2020/06/10)
Provided are 13-membered macrolides for the treatment of infectious diseases. The 13-membered macrolides described herein are azaketolides. Also provided are methods for preparing the 13- membered macrolides, pharmaceutical compositions comprising the 13-membered macrolides, and methods of treating infectious diseases, and in particular, disease resulting from Gram negative bacteria using the disclosed macrolides. Formula (I)
Design, synthesis and biological evaluation of novel tetrahydrothieno [2,3-c]pyridine substitued benzoyl thiourea derivatives as PAK1 inhibitors in triple negative breast cancer
Yao, Dahong,Huang, Jian,Wang, Jinhui,He, Zhendan,Zhang, Jin
, p. 1524 - 1538 (2020/08/07)
The overexpression of P21-activated kinase 1 (PAK1) is associated with poor prognosis in several cancers, which has emerged as a promising drug targets. Based on high-throughput virtual screening strategy, tetrahydrothieno [2,3-c]pyridine scaffold was identified as an initial lead for targeting PAK1. Herein we reported our structure-based optimisation strategy to discover a potent PAK1 inhibitor (7j) which displayed potent PAK1 inhibition and antiproliferatory activity in MDA-MB-231 cells. 7j induced obviously G2/M cell cycle arrest via PAK1-cdc25c-cdc2 pathway, and also inhibited MAPK-ERK and MAPK-JNK cascade to induce MDA-MB-231 cell death. Together, these results provided a novel chemical scaffold as PAK1 inhibitor for breast cancer treatment.