4591-55-3Relevant articles and documents
Identification and synthesis of novel alkaloids from the root system of Nicotiana tabacum: Affinity for neuronal nicotinic acetylcholine receptors
Wei, Xiaochen,Sumithran, Sangeetha P.,Deaciuc, A. Gabriela,Burton, Harold R.,Bush, Lowell P.,Dwoskin, Linda P.,Crooks, Peter A.
, p. 495 - 505 (2005)
A novel pyridine derivative, 3,5-bis-(1-methyl-pyrrolidin-2-yl)-pyridine, and a pair of diastereomers of 1,1′-dimethyl-[2,3′]bipyrrolidinyl were isolated from the root of Nicotiana tabacum plants and identified as novel alkaloids by GC-MS analysis. The structures of these new alkaloids were confirmed by total synthesis. The affinities of these novel alkaloids, and other structurally related compounds for α4β2*, α7* neuronal nicotinic acetylcholine receptors (nAChRs), and for nAChRs mediating nicotine-evoked dopamine release from rat striatum were also assessed. The results indicate that these compounds do not interact with α7* nAChRs, but inhibit [3H]nicotine binding to the α4β 2* nAChR subtype. The results also demonstrate that these compounds act as antagonists at nAChRs mediating nicotine-evoked dopamine release from rat striatum.
Bis-isatin hydrazones with novel linkers: Synthesis and biological evaluation as cytotoxic agents
Ibrahim, Hany S.,Abou-Seri, Sahar M.,Ismail, Nasser S.M.,Elaasser, Mahmoud M.,Aly, Mohamed H.,Abdel-Aziz, Hatem A.
, p. 415 - 422 (2016)
Many bis-isatins and isatins with hydrazide extension were reported to have a potential anti-proliferative effects against different cancer cell lines and cancer targets. In this study, four series of bis-isatins with hydrazide linkers were synthesized. These compounds were investigated for their antitumor activity by assessing their cytotoxic potency against HepG2, MCF-7 and HCT-116 cancer cell lines. Compound 21c possessed significant cytotoxic activity against MCF-7 (IC50 = 1.84 μM) and HCT-116 (IC50 = 3.31 μM) that surpasses the activity of doxorubicin against both cell lines (MCF-7; IC50 = 2.57 μM and HCT-116; IC50 = 3.70 μM). Cell cycle analysis and annexin V-FITC staining of MCF-7 cells treated with 21c suggested that the cytotoxic effect of the compound could be attributed to its pro-apoptotic activity.
Design, synthesis, and evaluation of 2-anilino-4-(3,5-dicarboxamidespiperidine)-pyrimidines as anaplastic lymphoma kinase inhibitors
Latif, Muhammad,Park, Sangjun,Ali, Imran,Choe, Hyeonjeong,Chae, Chong Hak,Park, Chi Hoon,Kim, Hyoung Rae,Yun, Chang-Soo,Lee, Kwangho
, p. 2397 - 2400 (2015)
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A predictive model for additions to: N -alkyl pyridiniums
Knight, Brian J.,Tolchin, Zachary A.,Smith, Joel M.
supporting information, p. 2693 - 2696 (2021/03/18)
Disclosed in this communication is a thorough study on the dearomative addition of organomagnesium nucleophiles to N-alkyl pyridinium electrophiles. The regiochemical outcomes have observable and predictable trends associated with the substituent patterns on the pyridinium electrophile. Often, the substituent effects can be either additive, giving high selectivities, or ablative, giving competing outcomes. Additionally, the nature of the organometallic nucleophilic component was also investigated for its role in the regioselective outcome. The effects of either reactive component are important to both the overall reactivity and site of nucleophilic addition. The utility of these observed trends is demonstrated in a concise, dearomative synthesis of a tricyclic compound shown to have insecticidal activity. This journal is
SMALL MOLECULES THAT SENSITIZE HIV-1 INFECTED CELLS TO ANTIBODY DEPENDENT CELLULAR CYTOTOXICITY
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Paragraph 0025, (2020/02/23)
Compounds and methods of treating HIV-1 in a human infected with HIV-1 or preventing HIV-1 infection in a human susceptible to infection with HIV-1 are provided. The compounds are of formula (I), (II), and (IA), wherein R1-R7, X, X', Y, Y', Z, and n are defined herein, and the methods comprises administering therapeutically effective amounts of these compounds to the human.
