1085708-84-4Relevant academic research and scientific papers
Design, synthesis and bioactivity evaluation of novel β-carboline 1,3,4-oxadiazole derivatives
Zhang, Zhi-Jun,Zhang, Jing-Jing,Jiang, Zhi-Yan,Zhong, Guo-Hua
, (2017)
A series of novel β-carboline 1,3,4-oxadiazole derivatives were designed and synthesized, and the in vitro cytotoxic activity against Sf9 cells and growth inhibitory activity against Spodoptera litura were evaluated. Bioassay results showed that most of these compounds exhibited excellent in vitro cytotoxic activity. Especially, compound 37 displayed the best efficacy in vitro (IC50 = 3.93 μM), and was five-fold more potent than camptothecin (CPT) (IC50 = 18.95μM). Moreover, compounds 5 and 37 could induce cell apoptosis and cell cycle arrest and stimulate Sf-caspase-1 activation in Sf9 cells. In vivo bioassay also demonstrated that compounds 5 and 37 could significantly inhibit larvae growth of S. litura with decreasing the weight of larvae and pupae. Based on these bioassay results, compounds 5 and 37 emerged as lead compounds for the development of potential insect growth inhibitions.
Banisterine oxazoline derivate and preparation method and application thereof
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Paragraph 0095; 0115-0117, (2016/11/28)
The invention discloses a banisterine oxazoline derivate and a preparation method and application thereof. The structural formula of the banisterine oxazoline derivate is shown in the formula (I), wherein R1 is methyl or phenyl or p-methylphenyl or p-chlorophenyl or p-bromophenyl or p-trifluoromethylphenyl or p-methoxyphenyl or 3,4,5-triethoxy phenyl or o-chlorophenyl or m-chlorobenzene or 2-naphthyl; R2 is sulfydryl or hydroxyl or azyl or ethyl or cyclopropyl or phenyl or p-methylphenyl or p-chlorphenyl. The derivate can have the remarkable cytotoxic activity for spodoptera frugiperda cell free system Sf9, and has the remarkable inhibitory activity for rhizoctonia solani. The banisterine oxazoline derivate is simple in structure, easy to synthesize, simple in synthesis technology, high in product purity and suitable for large-scale industrial production and has the good application prospect.
Synthesis and antitumoral activity of novel 3-(2-substituted-1,3,4-oxadiazol-5-yl) and 3-(5-substituted-1,2,4-triazol-3-yl) β-carboline derivatives
Formagio, Anelise S. Nazari,Tonin, Lilian T. Duesman,Foglio, Mary Ann,Madjarof, Christiana,de Carvalho, Joao Ernesto,da Costa, Willian Ferreira,Cardoso, Flavia P.,Sarragiotto, Maria Helena
experimental part, p. 9660 - 9667 (2009/04/06)
Several novel 1-substituted-phenyl β-carbolines bearing the 2-substituted-1,3,4-oxadiazol-5-yl and 5-substituted-1,2,4-triazol-3-yl groups at C-3 were synthesized and evaluated for their in vitro anticancer activity. The assay results pointed thirteen compounds with growth inhibition effect (GI50 50 values lying in the nanomolar concentration range (GI50 = 10 nM for both compounds). The 1-(N,N-dimethylaminophenyl)-3-(5-thioxo-1,2,4-triazol-3-yl) β-carboline (8g) was the most active compound, showing particular effectiveness on lung (GI50 = 0.06 μM), ovarian and renal cell lines. The potent anticancer activity presented for synthesized compounds 7a, 7h, and 8g, together with their easiness of synthesis, makes these compounds promising anticancer agents.
