30788-35-3Relevant articles and documents
Syntheses of deuterium-labelled cholesteryl neoglycolipids
Lafont, Dominique,Boullanger, Paul,Gambetta, Antoine
, p. 88 - 95 (2012)
Four deuterium-labelled neoglycolipids derived from cholesterol were synthesized for embedment into liposomes. Deuterium atoms were either incorporated by CH2 replacement with a CD2 group in the triethylene glycol spacer arm between the cholesteryl residue and the sugar moiety (products 2-4) or incorporated directly on the acetamido function in the sugar head (compound 5). Copyright
Apoptosis inducing properties of 3-biotinylate-6-benzimidazole B-nor-cholesterol analogues
Zhu, Zhiling,Liu, Zhiping,Cui, Jianguo,Huang, Yanmin,Chen, Hualong,Wu, Yulan,Huang, Xiaotong,Gan, Chunfang
, (2021)
In this work, a series of Biotin-substituted B-nor-cholesteryl benzimidazole compounds were synthesized. The antiproliferative activities of these compounds were evaluated in vitro using a series of human cancer cell lines, including HeLa (cervical cancer), SKOV3 (ovarian cancer), T-47D (thymus gland cancer), MCF-7 (human breast cancer) and HEK293T (normal renal epithelial) cells. These compounds displayed distinct antiproliferative activities against the currently tested cancer cells. The apoptotic properties induced by compound 6d were further investigated. Our results showed that compound 6d could induce the apoptosis of SKOV3 cells, blocking the cell growth in S-phase. Western blotting analyses revealed that compound 6d can induce cell apoptosis via the mitochondria-dependent pathway.
LIPIDIC ANALOGS OF ANTI-CANCER STEM CELL AGENT
-
, (2020/09/19)
A group of specific sulfated flavonoid agents carrying cholesterol modification display promising in vivo anti-cancer activity through selective inhibition of cancer stem cells, and not of adult or hematopoietic stem cells. The compounds exhibit high potency, excellent oral bioavailability and a physiologically relevant therapeutic window.
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.
3-biotin ether ester-B reduction-cholesteric benzimidazole compound and preparation method and application thereof
-
Paragraph 0043; 0048; 0052; 0057, (2019/01/16)
The invention discloses a 3-biotin ether ester-B reduction-cholesteric benzimidazole compound and a preparation method and application thereof. The 3-biotin ether ester-B reduction-cholesteric benzimidazole compound is characterized in that the chemical structure formula refers to the description, wherein n is an even number which is more than or equal to 2; R1 is H or CH3; R2 is H or OCH3. The 3-biotin ether ester-B reduction-cholesteric benzimidazole compound is obvious in effect on inhibiting cells of various tumor cell strains such as human uterine cervix cancer cell strains, ovarian carcinoma cell strains and human breast carcinoma cell lines; and meanwhile, the 3-biotin ether ester-B reduction-cholesteric benzimidazole compound is nontoxic to human renal epithelial cells and can be applicable to preparation of drugs for treating cancers.
Catalytic cyclometallation in steroid chemistry VI: Targeted synthesis of hybrid molecules based on steroids and tetradeca-5Z,9Z-diene-1,14-dicarboxylic acid and study of their antitumor activity
D'yakonov, Vladimir A.,Tuktarova, Regina A.,Dzhemileva, Lilya U.,Ishmukhametova, Svetlana R.,Yunusbaeva, Milyausha M.,Dzhemilev, Usein M.
, p. 6 - 13 (2018/06/18)
Hybrid molecules based on a number of steroids (cholesterol, pregnenolone, androsterone) and 1,14-tetradeca-5Z,9Z-dienedicarboxylic acid linked via mono- and diethylene glycol spacers were synthesized for the first time and studied for antitumor activity in vitro. The acid was prepared using catalytic cyclomagnesiation of oxygenated 1,2-dienes with Grignard reagent in the presence of Cp2TiCl2 as the key synthetic step. Using flow cytometry, the new molecules were shown for the first time to be efficient apoptosis inducers in the HeLa, Hek293, U937, Jurkat, and K562 cell cultures and to have dose-dependent effect on the S and G2 phases of the cell cycle.
FLUORESCENT ANTICANCER PLATINUM DRUGS
-
, (2018/11/21)
The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to fluorescent platinum based compounds. The disclosure further relates to synthesis of said fluorescent platinum based compounds, nanoparticles and compositions comprising said fluorescent platinum based compounds/nanoparticles. The disclosure also relates to methods of managing cancer by the fluorescence changes between aforesaid platinum based compounds and corresponding free ligands, nanoparticles and compositions.
CELLULAR SIGNALLING INHIBITORS, THEIR FORMULATIONS AND METHODS THEREOF
-
, (2017/09/05)
The present disclosure relates generally to Cellular Signalling inhibitors of compound of Formula (I), compositions and formulations comprising the same, methods, processes, and uses thereof. In particular, the present disclosure provides CSF-1R inhibitors demonstrating sustained inhibition of CSF/CSF1R signalling pathway with decreased toxicity. The present disclosure also provides supramolecular combinatorial therapeutics, wherein a CSF-1R inhibitor is combined with one or more of a chemotherapeutic agent, a kinase inhibitor, and an immunoregulator, each of which is optionally conjugated with a lipid. The present disclosure also provides a method for treating cancer, allergy, Systemic lupus erythematosus, nephritis, Chronic Obstructive Pulmonary Disease, and abnormal macrophage functions or any combinations thereof.
Hybrid Lipids Inspired by Extremophiles and Eukaryotes Afford Serum-Stable Membranes with Low Leakage
Koyanagi, Takaoki,Cao, Kevin J.,Leriche, Geoffray,Onofrei, David,Holland, Gregory P.,Mayer, Michael,Sept, David,Yang, Jerry
supporting information, p. 6757 - 6762 (2017/05/29)
This paper presents a new hybrid lipid that fuses the ideas of molecular tethering of lipid tails used by archaea and the integration of cholesterol groups used by eukaryotes, thereby leveraging two strategies employed by nature to increase lipid packing
BIPOLAR TETRAETHER LIPIDS
-
Paragraph 0034; 0569; 0570, (2017/03/21)
Disclosed herein, inter alia, are compounds, compositions, and liposomes and methods of thereof.