26089-39-4Relevant articles and documents
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.
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.
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