61130-13-0Relevant articles and documents
Substituted dienes prepared from betulinic acid – Synthesis, cytotoxicity, mechanism of action, and pharmacological parameters
Frydrych, Ivo,Urban, Milan,?arek, Jan,Benická, Sandra,D?ubák, Petr,Gurská, Soňa,Hajdúch, Marián,Kotulová, Jana,Li?ková, Barbora,Olejníková, Denisa,Pokorny, Jan
, (2021/07/28)
A set of new substituted dienes were synthesized from betulinic acid by its oxidation to 30-oxobetulinic acid followed by the Wittig reaction. Cytotoxicity of all compounds was tested in vitro in eight cancer cell lines and two noncancer fibroblasts. Almost all dienes were more cytotoxic than betulinic acid. Compounds 4.22, 4.30, 4.33, 4.39 had IC50 below 5 μmol/L; 4.22 and 4.39 were selected for studies of the mechanism of action. Cell cycle analysis revealed an increase in the number of apoptotic cells at 5 × IC50 concentration, where activation of irreversible changes leading to cell death can be expected. Both 4.22 and 4.39 led to the accumulation of cells in the G0/G1 phase with partial inhibition of DNA/RNA synthesis at 1 × IC50 and almost complete inhibition at 5 × IC50. Interestingly, compound 4.39 at 5 × IC50 caused the accumulation of cells in the S phase. Higher concentrations of tested drugs probably inhibit more off-targets than lower concentrations. Mechanisms disrupting cellular metabolism can induce the accumulation of cells in the S phase. Both compounds 4.22 and 4.39 trigger selective apoptosis in cancer cells via intrinsic pathway, which we have demonstrated by changes in the expression of the crucial apoptosis-related protein. Pharmacological parameters of derivative 4.22 were superior to 4.39, therefore 4.22 was the finally selected candidate for the development of anticancer drug.
ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES
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Paragraph 0191, (2019/02/25)
A compound having a structure of the formula Ir(LA)(LB), in which LA is a bidentate, tridentate, tetradentate, pentadentate, or hexadentate ligand and LB is a monodentate, bidentate, tridentate, or tetradentate ligand, or not present, and where the total denticity of LA plus LB is 6, and LA includes at least one structure of Formula I: is disclosed as a useful phosphorescent emitter compound.
PHENACENE COMPOUND, METHOD FOR PRODUCING PHENACENE COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT
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Paragraph 0176; 0177, (2017/11/01)
PROBLEM TO BE SOLVED: To provide a phenacene compound having a high fluorescence yield. SOLUTION: The present invention provides a phenacene compound represented by formula (1), where A is a group represented by formula (2); Z1 and Z2/sup
Investigation of pyrolysis temperature in the one-step synthesis of L10 FePt nanoparticles from a FePt-containing metallopolymer
Dong, Qingchen,Li, Guijun,Wang, Hua,Wing-Tat Pong, Philip,Leung, Chi-Wah,Manners, Ian,Ho, Cheuk-Lam,Li, Hua,Wong, Wai-Yeung
, p. 734 - 741 (2015/07/27)
Ferromagnetic (L10 phase) FePt alloy nanoparticles (NPs) with extremely high magnetocrystalline anisotropy are considered to be very promising candidates for the next generation of ultrahigh-density data storage systems. The question of how to generate L10 FePt NPs with high coercivity, controllable size, and a narrow size distribution is a challenge. We report here a single-step fabrication of L10 FePt NPs by employing one of the two new polyferroplatinyne bimetallic polymers as precursors. The influence of the pyrolysis temperature on the size and magnetic properties of the resulting FePt alloy NPs has been investigated in detail.
N-HYDROXY BICYCLIC HYDANTOIN CARBAMATES AS TOOLS FOR IDENTIFICATION OF SERINE HYDROLASE TARGETS
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Paragraph 00386, (2016/03/08)
Provided herein are N-hydroxy bicyclic hydantoin carbamates and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of serine hydrolases. Furthermore, the subject compounds and composition
Bestowing structure upon the pores of a supramolecular network
Karamzadeh, Baharan,Eaton, Thomas,Cebula, Izabela,Torres, David Muoz,Neuburger, Markus,Mayor, Marcel,Buck, Manfred
supporting information, p. 14175 - 14178 (2015/01/09)
Trigonal molecules compartmentalise the pores of a honeycomb network of 3,4:9,10-tetracarboxylic diimide (PTCDI) and 1,3,5-triazine-2,4,6-triamine (melamine). Extending the 1,3,5-tri(phenylene-ethynylene)benzene core by a phenyl group allows for a well-defined accommodation of the molecule into two symmetry equivalent positions in the pore. The corresponding styryl or phenylene-ethynylene derivatives exceed the pore size and, thus, impede pore modification. This journal is
Ferrocenyl pyrazaboles: Design, synthesis, structure, and properties
Misra, Rajneesh,Jadhav, Thaksen,Mobin, Shaikh M.
, p. 2013 - 2022 (2014/01/17)
This article reports the design and synthesis of donor-acceptor-donor type ferrocenyl-substituted pyrazaboles by the Pd-catalyzed Suzuki and Sonogashira coupling reactions. The photophysical and electrochemical behaviors of the ferrocenyl-substituted pyra
Synthesis of 2-phenylnaphthalenes from styryl-2-methoxybenzenes
Mudududdla, Ramesh,Sharma, Rohit,Abbat, Sheenu,Bharatam, Prasad V.,Vishwakarma, Ram A.,Bharate, Sandip B.
supporting information, p. 12076 - 12079 (2015/02/19)
A new simple and efficient method for the synthesis of 2-phenylnaphthalenes from electron-rich 1-styryl-2-methoxybenzenes has been described. The reaction proceeds via TFA catalyzed C-C bond cleavage followed by intermolecular [4+2]-Diels-Alder cycloaddition of an in situ formed styrenyl trifluoroacetate intermediate. The quantum chemical calculations identified the transition state for the cycloaddition reaction and helped in tracing the reaction mechanism. The method has been efficiently utilized for synthesis of the phenanthrene skeleton and a naphthalene-based potent and selective ER-β agonist. This journal is
A detailed kinetic analysis of rhodium-catalyzed alkyne hydrogenation
Luo, Jingwei,Oliver, Allen G.,Scott McIndoe
, p. 11312 - 11318 (2013/08/23)
Continuous monitoring using electrospray ionisation mass spectrometry (ESI-MS) shows that Wilkinson's catalyst hydrogenates a charge-tagged alkyne to the corresponding alkene, and at only a marginally slower rate, to the alkane. No rhodium-containing inte
Design, synthesis, in vitro cytotoxicity evaluation and structure-activity relationship of Goniothalamin analogs
Mohideen, Mazlin,Zulkepli, Suraya,Nik-Salleh, Nik-Salmah,Zulkefeli, Mohd,Weber, Jean-Frédéric Faizal Abdullah,Rahman, A. F. M. Motiur
, p. 812 - 831 (2013/07/26)
A series of six/five member (E/Z)-Goniothalamin analogs were synthesized from commercially available (3,4-dihydro-2H-pyran-2-yl)methanol/5- (hydroxymethyl)dihydrofuran-2(3H)-one in three steps with good to moderate overall yields and their cytotoxicity against lymphoblastic leukemic T cell line (Jurkat E6.1) have been evaluated. Among the synthesized analogs, (Z)-Goniothalamin appeared to be the most active in cytotoxicity (IC 50 = 12 μM). Structure-activity relationship study indicates that introducing substituent in phenyl ring or replacing phenyl ring by pyridine/naphthalene, or decreasing the ring size of lactones (from six to five member) do not increase the cytotoxicity.
