19434-65-2Relevant academic research and scientific papers
New series of double-modified colchicine derivatives: Synthesis, cytotoxic effect and molecular docking
Aminpour, Maral,Huczyn?ski, Adam,Krzywik, Julia,Maj, Ewa,Mozga, Witold,Tuszyn?ski, Jack A.,Wietrzyk, Joanna
, (2020)
Colchicine is a well-known anticancer compound showing antimitotic effect on cells. Its high cytotoxic activity against different cancer cell lines has been demonstrated many times. In this paper we report the syntheses and spectroscopic analyses of novel colchicine derivatives obtained by structural modifications at C7 (carbon-nitrogen single bond) and C10 (methylamino group) positions. All the obtained compounds have been tested in vitro to determine their cytotoxicity toward A549, MCF-7, LoVo, LoVo/DX, and BALB/3T3 cell lines. The majority of obtained derivatives exhibited higher cytotoxicity than colchicine, doxorubicin and cisplatin against the tested cancerous cell lines. Additionally, most of the presented derivatives were able to overcome the resistance of LoVo/DX cells. Additionally, their mode of binding to β-tubulin was evaluated in silico. Molecular docking studies showed that apart from the initial amides 1 and 2, compound 14, which had the best antiproliferative activity (IC50 = 0.1–1.6 nM), stood out also in terms of its predicted binding energy and probably binds best into the active site of βI-tubulin isotype.
ANTIMICROBIAL COMPOSITIONS, METHODS OF MAKING, AND METHODS OF USE
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Paragraph 0011; 0013, (2019/03/08)
The invention provides a protected antimicrobial compound and methods of using the same.
Acid-Triggered, Acid-Generating, and Self-Amplifying Degradable Polymers
Miller, Kali A.,Morado, Ephraim G.,Samanta, Shampa R.,Walker, Brittany A.,Nelson, Arif Z.,Sen, Samya,Tran, Dung T.,Whitaker, Daniel J.,Ewoldt, Randy H.,Braun, Paul V.,Zimmerman, Steven C.
supporting information, p. 2838 - 2842 (2019/03/05)
We describe the 3-iodopropyl acetal moiety as a simple cleavable unit that undergoes acid catalyzed hydrolysis to liberate HI (pKa-10) and acrolein stoichiometrically. Integrating this unit into linear and network polymers gives a class of macromolecules that undergo a new mechanism of degradation with an acid amplified, sigmoidal rate. This trigger-responsive self-amplified degradable polymer undergoes accelerated rate of degradation and agent release.
PROTECTED CARBOXYLIC ACID-BASED METABOLITES FOR THE TREATMENT OF MITOCHONDRIAL DISORDERS
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Page/Page column 50, (2017/07/29)
The present invention provides novel cell-permeable carboxylic acid-based metabolites and cell permeable precursors thereof aimed at increasing ATP-production in mitochondria. The main part of ATP produced and utilized in the eukaryotic cell originates fr
METHOD FOR THE CATALYTIC REDUCTION OF ACID CHLORIDES AND IMIDOYL CHLORIDES
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Paragraph 0104, (2014/08/19)
The present application relates to methods for the catalytic reduction of acid chlorides and/or imidoyl chlorides. The methods comprise reacting the acid chloride or imidoyl chloride with a silane reducing agent in the presence of a catalyst such as [Cp(Pri3P)Ru(NCMe)2]+[PF6]?.
Chemoselective ruthenium-catalyzed reduction of acid chlorides to aldehydes with dimethylphenylsilane
Gutsulyak, Dmitry V.,Nikonov, Georgii I.
experimental part, p. 607 - 611 (2012/04/23)
A variety of aromatic and alkyl acid chlorides can be selectively converted into aldehydes using dimethylphenyl silane (HSiMe2Ph) as the reducing reagent in the presence of the cationic ruthenium catalyst {Cp[(i-Pr)3P]Ru(NCMe)2}+ [PF6] -. The reactions proceed under very mild conditions and are tolerant to many functional groups. Copyright
Intermolecular oxonium ylide mediated synthesis of medium-sized oxacycles
MacK, Daniel J.,Batory, Lindsay A.,Njardarson, Jon T.
supporting information; experimental part, p. 378 - 381 (2012/03/09)
Detailed in this account are our efforts toward efficient oxacycle syntheses. Two complementary approaches are discussed, with both employing chemoselective allyl ether activation and rearrangement as the key step. Vinyl substituted oxiranes and oxetanes provide a single step access to dihydropyrans and tetrahydrooxepines. Oxiranes proved to be poor substrates, while oxetanes were slightly better. An alternative approach using substituted allyl ethers proved successful and addressed the limitations encountered in the ring expansions.
Amido macrolides
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, (2008/06/13)
Various macrolide compounds such as those having the following formulas are provided where the variables have the values provided herein.
Amido macrolides
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Page/Page column 25, (2010/01/31)
Various macrolide compounds such as those having the following formulas are provided where the variables have the values provided herein.
N-(4-methylbenzenesulfonyl)- pyrrolidines and piperidines by a tandem S(N)2-Michael addition reaction
Bunce, Richard A.,Allison, Jeffrey C.
, p. 2175 - 2186 (2007/10/03)
A tandem S(N)2-Michael addition sequence has been developed for the preparation of N-(4-methylbenzenesulfonyl)- pyrrolidines and piperidines bearing functionalized side chains at C-2.
