26089-39-4Relevant academic research and scientific papers
Radio-opaque theranostic nanoemulsions with synergistic anti-cancer activity of paclitaxel and Bcl-2 siRNA
Oh, Mi Hwa,Kim, Jee Seon,Lee, Jeong Yu,Park, Tae Gwan,Nam, Yoon Sung
, p. 14642 - 14651 (2013)
The integration of therapeutic and imaging functions in a nanoscale structure is gaining increasing attention to monitor drug and gene delivery in a non-invasive real-time manner. Here we introduce radio-opaque nanoemulsions incorporating paclitaxel and Bcl-2 small interfering RNA (siRNA) for synergistic anti-cancer theranostics. Water-insoluble paclitaxel is readily dissolved in iodinated poppy seed oil (Lipiodol) and emulsified in an aqueous solution using a mixture of PEGylated phospholipids, cholesterols, and linear polyethylenimine grafted with cholesterols. The prepared cationic nanoemulsions were electrostatically complexed with Bcl-2 siRNA for the co-delivery of paclitaxel and siRNA, inducing a dramatically higher level of apoptosis and cytotoxic activity in breast adenocarcinoma compared to individual treatments. The feasibility of the nanoemulsions for bio-imaging applications is preliminarily investigated using micro-computed tomography with a mouse model. This study suggests that the Lipiodol nanoemulsions can be used as a multifunctional nanocarrier platform for the co-delivery of anti-cancer drugs and siRNA with bio-imaging functionality to efficiently increase the modality of anti-cancer theranostics. The Royal Society of Chemistry 2013.
Glucosamine-6-phosphate synthase inhibiting C3-β-cholesterol tethered spiro heterocyclic conjugates: Synthesis and their insight of DFT and docking study
Periyasami, Govindasami,Kamalraj, Subban,Padmanaban, Ramanathan,Yeswanth Kumar, Santhakumar,Stalin, Antony,Arumugam, Natarajan,Suresh Kumar, Raju,Rahaman, Mostafizur,Durairaju, Periyan,Alrehaili, Abdulaziz,Aldalbahi, Ali
, (2019)
A series of novel covalent cholesterol-spiro pyrrolidine/pyrrolizidine heterocyclic hybrids possessing biologically active oxindole, indanedione, and acenaphthylene-1-one have been synthesized by the reaction of C3-β-cholesteroalacrylate with heterocyclic
Trifluoromethyl allyl compound as well as preparation method and application thereof
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Paragraph 0046-0050, (2021/08/06)
The invention discloses a trifluoromethyl allyl compound as well as a preparation method and application thereof. According to the method, allyl alcohol is directly used as a raw material, CF3SO2Na is selected as a trifluoromethylation reagent, a metal-free and cheap photooxidation reduction catalyst is used, and under the catalysis of an organic photooxidation reduction agent, a byproduct SO2 generated in situ is reused as an activated C-OH bond, so that the reaction is carried out in an environment-friendly manner under a mild condition. The allyl alcohol used in the preparation method disclosed by the invention is a MoritA-Baylis-Hillman alcohol allyl alcohol raw material which is simple to synthesize and high in conversion rate, the applicable substrate range is wide, and the preparation cost is low. In addition, the preparation method disclosed by the invention is simple in steps, and has the characteristics of convenience in operation, environment friendliness, excellent stereoselectivity and broad-spectrum functional group tolerance. The trifluoromethyl allyl compound provided by the invention is a general precursor for preparing related CF3 molecules, has potential pharmaceutical activity and biological activity, and can be widely applied to biological and pharmaceutical active molecules.
Acid- And base-switched palladium-catalyzed γ-C(sp3)-H alkylation and alkenylation of neopentylamine
Zhang, Jinquan,Zhang, Shuaizhong,Zou, Hongbin
supporting information, p. 3466 - 3471 (2021/05/31)
The functionalization of remote unactivated C(sp3)-H and the reaction selectivity are among the core pursuits for transition-metal catalytic system development. Herein, we report Pd-catalyzed γ-C(sp3)-H-selective alkylation and alkenylation with removable 7-azaindole as a directing group. Acid and base were found to be the decisive regulators for the selective alkylation and alkenylation, respectively, on the same single substrate under otherwise the same reaction conditions. Various acrylates were compatible for the formation of C(sp3)-C(sp3) and C(sp3)-C(sp2) bonds. The alkenylation protocol could be further extended to acrylates with natural product units and α,β-unsaturated ketones. The preliminary synthetic manipulation of the alkylation and alkenylation products demonstrates the potential of this strategy for structurally diverse aliphatic chain extension and functionalization. Mechanistic experimental studies showed that the acidic and basic catalytic transformations shared the same six-membered dimer palladacycle.
Ru(II)-Catalyzed Oxidative Olefination of Benzamides: Switchable Aza-Michael and Aza-Wacker Reaction for Synthesis of Isoindolinones
Kumar, Manoj,Verma, Akhilesh K.,Verma, Shalini
supporting information, (2020/06/25)
Selective tandem oxidative C-H olefination-aza-Michael/aza-Wacker reaction of N-arylbenzamides is achieved by fine-tuning between base and additive to access valuable 3-oxoisoindolinyls and 3-oxoisoindolinylidenes, respectively. Careful optimization and c
Self-organization of cholesterol-side-chain liquid crystalline polymers by tailoring the main chain structure and flexible spacer length
Yang, Xiwen,Chen, Shaonan,Luo, Hang,Xu, Haoran,Chen, Sheng
, p. 5429 - 5440 (2019/04/04)
Three kinds of side-chain liquid crystalline polymers (SCLCPs), in which cholesteryl mesogens (Chol) were linked to polyacrylate (PCholAC-m), polymethacrylate (PCholMC-m), and poly(2-vinylbenzene-1,4-dioate) (PCholVA-m) backbones through methylene spacers of different lengths (m = 0, 2, 4, 6, 8, and 10), were successfully synthesized using free-radical polymerization. The phase behavior and structure of the polymers were investigated in detail using DSC, POM, and SAXS. The results indicated that the Chol-SCLCPs displayed interesting self-organization by varying the main-chain structure and spacer length. The polymers initially form a smectic A phase, except for PCholAC-0 without a liquid crystalline phase. Next, polymers PCholAC-m (m = 2, 4, 6) formed a two-layer smectic A phase in which the alkyl tail was overlapped (SmA2). Two-phase coexisting structures were observed in PCholAC-m (m = 8, 10), including a bilayer smectic A phase in which the alkyl tail was inserted into the mesogens (SmAd) and a single-layer smectic A phase in which the mesogens were overlapped (SmA1). Similar results were observed for PCholMC-m. Furthermore, PCholMC-0 possessed a stable bilayer SmA2 owing to the methyl steric effect of the main chain. PCholVA-m (m = 0, 2, 4) samples showed a well-defined smectic A phase in which the backbone was squeezed by the parallel side chains on both sides. PCholVA-6 and PCholVA-10 exhibited a SmAd phase. The two-phase coexisting structures were also found in PCholVA-8. Finally, the glass transition temperature of the polymers decreased with increasing flexible spacer length because the flexible spacer acted as an internal plasticizer in the system. However, changes in the polymer clearing points demonstrated the diversity resulting from the different smectic A phase structures.
FORMULATIONS FOR THE DELIVERY OF ACTIVE AGENTS TO INSECTS, PLANTS, AND PLANT PATHOGENS
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Paragraph 0283; 0284, (2017/12/07)
The present disclosure is directed to formulations comprising (1) at least one formulation transport agent, (2) at least one complexing agent, and (3) at least one active agent that modulates one or more traits of a target insect, plant, or plant pathogen. The present disclosure is also directed to methods of delivering such formulations to the target organism, as well as to formulation transport agents used to prepare such formulations.
Synthesis of sialic-acid-group-containing lipid derivatives and application of sialic-acid-group-containing lipid derivatives in pharmaceutical preparations
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Paragraph 0116; 0117; 0118; 0119; 0120; 0121; 0122, (2017/06/28)
The invention provides sialic-acid-group-containing lipid derivatives which are widely used for particle preparation modification. The structure is disclosed as Formula (1), wherein R1 represents one of -OH, -HNCOCH3 and -NHCOCH2OH; the HN-R2-S segment is from SH-R2-NH2; SH-R2-NH2 is a compound containing primary amino group and mercapto group; the R3 segment is from compounds containing alpha,beta-unsaturated conjugated carbonyl; and the R4 segment is from R4-H which is a compound containing hydroxy or primary amino group. The sialic-acid-group-containing lipid derivatives provided by the invention can be used for surface modification of multiple particle preparations, and endow the modification preparation with the targeted distribution capacity.
Synthesis of sulfonated cholesterol derivatives - Electrical, thermal, and optical properties
Hoque, Samiul,Dass, Narendra Nath,Bhattacharyya, Krishna Gopal,Sarma, Neelotpal Sen
, p. 149 - 162 (2014/05/20)
Poly(cholesterylacrylatesulfone) (PCHAS) and poly(cholesterylacrylatesulfone-co-1-hexene)s (PCHASHs) at different ratios are synthesized from the monomer cholesteryl acrylate. The liquid crystalline phases are observed under a hot stage fitted with a polarizing optical microscope. The polysulfone and copolysulfones are characterized by FT-IR, 1H-NMR, DSC, and TGA techniques. From SEM (EDX) the qualitative amounts of elemental sulfur found in PCHAS and PCHASH11 are 2.90 weights (%) and 4.39 weights (%), respectively. The GPC data using THF as the solvent shows that the number average molecular weight of the PCHAS is 5268 g/mol and the molecular weights of the PCHASHs are higher than the PCHAS. Copyright Taylor & Francis Group, LLC.
1, 3-dichloro trifluoromethylbenzal manufacturing method
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, (2007/10/14)
Epichlorohydrin is produced from acetone by (1) chlorinating acetone to form monochloroacetone; (2) disproportionating the monochloroacetone in the presence of a platinum catalyst, a strong acid and preferably a chloride source (for example, added as a salt or from hydrolysis of monochloroacetone) and some water to produce acetone and 1,3-dichloroacetone; (3) hydrogenating the 1,3-dichloroacetone in the presence of a catalyst to produce 1,3-dichlorohydrin; and (4) cyclizing the 1,3-dichlorohydrin with a base to produce epichlorohydrin.
