1829-28-3Relevant academic research and scientific papers
Synthesis of E-stilbene azomethines as potent antimicrobial and antioxidant agents
Iqbal, Ahsan,Khan, Zulfiqar Ali,Shahzad, Sohail Anjum,Usman, Muhammad,Khan, Shakeel Ahmad,Fauq, Abdul H.,Bari, Ayesha,Sajid, Muhammad Aamir
, p. 1518 - 1533 (2018)
A series of new extensively conjugated E -stilbene azomethines (5a–5h) were synthesized and screened for their antioxidant and antimicrobial activity. The compounds were tested against bacterial (Escherichia coli, Staphylococcus aureus, Klebsiella pneumon
Synthesis and evaluation of antitumor activity of dibenzodiazepine derivatives
Cao, Ke,Yan, Jianwei,Yan, Fulin,Yin, Tiantian
, p. 1111 - 1122 (2021)
Abstract: A series of dibenzodiazepine 2-position derivatives, bearing N-methylpiperazine at the C-11 position, were prepared by using a concise approach. Their inhibitory activities of tumor cell proliferation in vitro were tested in five cell lines, including breast cancer cell BCAP37, gastric cancer cell SGC7901, liver cancer cell HepG2, cervical cancer cell HeLa and acute promyelocytic leukemia cell HL-60. Several compounds showed efficient tumor activity with IC50 values down to 0.30?μM. These compounds are expected to be a new class of potential anticancer lead compounds. Graphic abstract: [Figure not available: see fulltext.]
Synthesis and antiproliferative activity of substituted benzopyranoisoindoles: A new class of cytotoxic compounds
Hadjipavlou, Christiana,Kostakis, Ioannis K.,Pouli, Nicole,Marakos, Panagiotis,Pratsinis, Harris,Kletsas, Dimitris
, p. 4822 - 4825 (2006)
A series of novel aminosubstituted benzopyranoisoindoles possessing structural analogy to an active nitracrine metabolite are reported. The compounds exhibited interesting cytotoxic activity against a panel of cell lines, which was maximized by the presen
Synthesis, spectroscopic and computational evaluation of a xanthene-based fluorogenic derivatization reagent for the determination of primary amines
Barnoin, Guillaume,Burger, Alain,Dotsikas, Yannis,Gikas, Evagelos,Kalampaliki, Amalia D.,Kostakis, Ioannis K.,Le, Hoang-Ngoan,Mallick, Suman,Michel, Beno?t Y.,More, Yogesh W.,Vincent, Steve
, (2021)
To detect an analyte, typically at the sub-nanomolar scale, extremely sensitive analytical tools are required. Fluorescence is the spectroscopy of choice to achieve such a level due to its non-invasive nature and efficiency in accurately probing the sub-n
Synthesis, modeling studies and evaluation of E-stilbene hydrazides as potent anticancer agents
Iqbal, Ahsan,Khan, Zulfiqar Ali,Shahzad, Sohail Anjum,Ahmad Khan, Shakeel,Raza Naqvi, Syed Ali,Bari, Ayesha,Amjad, Hira,Umar, Muhammad Ihtisham
, p. 271 - 281 (2019)
A group of new thermodynamically more stable E-2-styrylbenzohydrazide derivatives (5a-i) were synthesized via palladium catalyzed Mizoroki-Heck reaction conditions. All synthesized compounds were characterized by UV-visible, FT-IR, 1H NMR, sup
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
Preparation of Functionalized Diorganomagnesium Reagents in Toluene via Bromine or Iodine/Magnesium-Exchange Reactions
Desaintjean, Alexandre,Danton, Fanny,Knochel, Paul
supporting information, p. 4461 - 4476 (2021/08/13)
A wide range of polyfunctionalized di(hetero)aryl- and dialkenyl-magnesium reagents are prepared in toluene within 10 to 120 minutes between 78 C and 25 C via an I/Mg- or Br/Mg-exchange reaction using reagents of the general formula R2Mg (R = sBu, Mes). Highly sensitive functional groups, such as triazene or nitro, are tolerated in these exchange reactions, enabling the synthesis of various functionalized (hetero)arene and alkene derivatives after quenching with several electrophiles including allyl bromides, acyl chlorides, aldehydes, ketones, and aryl iodides.
Ynoate-Initiated Selective C-N Esterification of Tertiary Amines under Transition-Metal and Oxidant-Free Conditions
Sun, Feixiang,Feng, Huangdi,Huang, Liliang,Huang, Junhai
supporting information, p. 713 - 717 (2021/01/14)
An efficient and selective method for metal-and oxidant-free deaminated esterification of tertiary amines is presented. In this protocol, ynoates play a key role to activate the Csp 3-N bond through a process of in situ generation of zwitterionic salts. The transformations show that Csp 3-N bond in the zwitterionic species has a lower dissociation energy than Csp 2-N bond, leading to break preferentially and be trapped by carboxylic acids to generate the corresponding products in moderate to good yield.
Lipshutz-type bis(amido)argentates for directed: Ortho argentation
Tezuka, Noriyuki,Hirano, Keiichi,Peel, Andrew J.,Wheatley, Andrew E. H.,Miyamoto, Kazunori,Uchiyama, Masanobu
, p. 1855 - 1861 (2020/03/03)
Bis(amido)argentate (TMP)2Ag(CN)Li2 (3, TMP-Ag-ate; TMP = 2,2,6,6-tetramethylpiperidido) was designed as a tool for chemoselective aromatic functionalization via unprecedented directed ortho argentation (DoAg). X-Ray crystallographic analysis showed that 3 takes a structure analogous to that of the corresponding Lipshutz cuprate. DoAg with this TMP-Ag-ate afforded multifunctional aromatics in high yields in processes that exhibited high chemoselectivity and compatibility with a wide range of functional groups. These included organometallics- A nd transition metal-susceptible substituents such as methyl ester, aldehyde, vinyl, iodo, (trifluoromethanesulfonyl)oxy and nitro groups. The arylargentates displayed good reactivity with various electrophiles. Chalcogen (S, Se, and Te) installation and azo coupling reactions also proceeded efficiently.
Synthesis and antimicrobial activity of new prenylated 2-pyrone derivatives
Chukwujekwu, Jude C.,Obi, Grace,van Heerden, Fanie R.
, (2020/02/11)
A series of new monoprenylated and diprenylated 2-pyrone derivatives with different halogen substituents were synthesized from the corresponding 6-aryl-4-hydroxy-2-pyrones by prenylation reactions. The compounds were evaluated for antibacterial activity and displayed significant in vitro activity with the highest activity shown by the monoprenylated 6-aryl-2-pyrones. All the compounds except the bromine-containing analogs were active against one or more tested bacteria, with Escherichia coli being the most susceptible of the test organisms. With the remarkable antibacterial activity of eight of the compounds against a drug-resistant β-lactamase-producing Klebsiella pneumoniae, a synergistic evaluation between each of these compounds and ampicillin was undertaken. Out of the eight combinations studied, synergistic effects were observed with two compounds, 4-(3-methylbut-2-enoxy)-6-phenyl-2H-pyran-2-one and 6-(4-fluorophenyl)-4-(3-methylbut-2-enoxy)-2H-pyran-2-one. Both compounds, at half the individual MIC values, were able to lower the MIC of ampicillin in combinations from 2500 to 2.4 μg/mL (1/1041 of MIC).
