118220-72-7Relevant articles and documents
New Scaffold for Angiogenesis Inhibitors Discovered by Targeted Chemical Transformations of Wondonin Natural Products
Yu, Shuai,Oh, Jedo,Li, Feng,Kwon, Yongseok,Cho, Hyunkyung,Shin, Jongheon,Lee, Sang Kook,Kim, Sanghee
, p. 1066 - 1071 (2017)
The structure of wondonin marine natural products was renovated to attain new drug-like scaffolds. Wondonins have novel antiangiogenic properties without overt cytotoxicity. However, the chemical instability and synthetic complexity of wondonins have hindered their development as a new type of antiangiogenesis agent. Using a structure-based bioisosterism, the benzodioxole moiety was changed to benzothiazole, and the imidazole moiety was replaced by 1,2,3-triazole. Our efforts resulted in a new scaffold with enhanced antiangiogenic activity and minimized cytotoxicity. One compound with this scaffold effectively inhibited hyaloid vessel formation in diabetic retinopathy mimic zebrafish model. The biological findings together suggested the potential of the scaffold as a lead structure for development of antiangiogenic drugs with novel functions and as a probe to elucidate new biological mechanisms associated with angiogenesis.
ALKALOID DERIVATIVE HAVING ANGIOGENESIS INHIBITORY EFFECT, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
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Paragraph 0039-0041, (2020/06/23)
The present invention relates to an alkaloid derivative inhibiting angiogenesis and having structural stability, and pharmaceutical composition comprising the same as an active ingredient. The alkaloid derivative of the present invention can be effectively used for treating or preventing diabetic retinopathy, cancer, duodenal ulcer, arthritis or obesity.
Cu-Catalyzed Direct C-P Bond Formation through Dehydrogenative Cross-Coupling Reactions between Azoles and Dialkyl Phosphites
Hore, Soumyadip,Srivastava, Abhijeet,Singh, Ravi P.
, p. 6868 - 6878 (2019/06/14)
A direct dehydrogenative cross-coupling of azoles [C(sp2)-H] with dialkyl phosphites [P(O)-H] to access 2-phosphonated azoles using Cu(I)/Cu(II) as catalyst and K2S2O8/di-tert-butylperoxide as oxidant has been achieved. A remarkable advantage over reported procedures includes that oxazoles, imidazoles, benz(ox/othi/imid)azoles, and indole are found to react under optimized reaction conditions to provide corresponding adducts in high yields. The mechanistic insight of cross-coupling was obtained by deuterium kinetic isotope effect studies.
Method for synthesizing benzothiazole by microwave radiation of benzothioamide compound in aqueous phase
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Paragraph 0013; 0080, (2019/02/13)
The invention discloses a method for synthesizing benzothiazole by microwave radiation of a benzothioamide compound in an aqueous phase. The method includes the steps: adding the benzothioamide compound into the aqueous phase under microwave conditions; performing cyclization under alkaline conditions to generate the benzothiazole. The method for preparing the benzothiazole is environmentally friendly, simple and convenient in operation, safe, cheap and efficient. Compared with the prior art, the method is applicable to a lot of functional groups, high in yield, few in by-products, simple in operation, safe, low in cost and environmentally friendly.
Synthesis of benzothiazoles from 2-aminobenzenethiols in the presence of a reusable polythiazolium precatalyst under atmospheric pressure of carbon dioxide
Chun, Supill,Yang, Sabyuk,Chung, Young Keun
, p. 3438 - 3442 (2017/05/31)
Synthesis of benzothiazoles from 2-aminobenzenethiols and carbon dioxide was carried out using poly(3,4-dimethyl-5-vinylthiazolium) iodide as a precatalyst to in situ generation of NHCs by deprotonation. The reaction was successfully carried out under mild conditions (1 atm of CO2 and 60–70 °C) with a broad substrate scope and functional group tolerance. The precatalyst salt was recovered and reused for several times without any loss of activity.
