Tag: 173.17

Synthesis and anticancer activity of novel quinoline-docetaxel analogues was written by Chen, Ming;Chen, Hui;Ma, Jiangwei;Liu, Xueying;Zhang, Shengyong. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2014.Application of 486-73-7 This article mentions the following:

A series of novel quinoline-docetaxel analogs I (R = 2-quinolinylcarbonyl, 3-quinolinylcarbonyl, 1-isoquinolinylcarbonyl, 6-quinolinylcarbonyl, etc., R¹ = H, COMe) were designed and synthesized by introducing bioactive quinoline scaffold to C2′-OH of docetaxel. The anticancer activities of these novel analogs were investigated against different human cancer cell lines including Hela, A549, A2780, MCF-7 and two resistant strains A2780-MDR and MCF-7-MDR. The data showed these analogs possessed similar to better cytotoxicity than docetaxel. Compound I (R = 6-quinolinyl, R¹ = H) was found to be the most potent one, and its IC₅₀ value against MCF-7-MDR was 8.8 nM (IC₅₀ of docetaxel was 180 nM). This work indicated that the introduction of quinolyl group in docetaxel could enhance cytotoxicity and reduce drug-resistance. In the experiment, the researchers used many compounds, for example, Isoquinoline-1-carboxylic acid (cas: 486-73-7Application of 486-73-7).

Isoquinoline-1-carboxylic acid (cas: 486-73-7) belongs to isoquinoline derivatives. The isoquinoline structure occurs in a considerable number of alkaloids in widely separated plant families. The discovery of chloroquine, the most well-known drug containing this stent, has helped bring about decades of malaria control and treatment.Application of 486-73-7

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem

Synthesis and study of substituted amides of isoquinoline-3- and isoquinoline-1-carboxylic acids as potential anticonvulsants was written by Strupinska, Marzanna;Rostafinska-Suchar, Grazyna;Jakubowicz, Bartlomiej;Klimkiewicz, Paulina;Lal, Ewelina;Oczkowski, Mateusz;Prochniak, Ewa;Pirianowicz-Chaber, Elzbieta;Mazurek, Aleksander P.. And the article was included in Acta Poloniae Pharmaceutica in 2017.Reference of 486-73-7 This article mentions the following:

Previously obtained benzylamides of isoquinoline-3-carboxylic acids and isoquinoline-1-carboxylic acids exhibited anticonvulsant activity. In search for more effective anticonvulsants, a series of amides of isoquinoline- 3- and isoquinoline-1-carboxylic acids have been synthesized (1-9). The obtained compounds were evaluated qual. for their anticonvulsant activity in the maximal electroshock seizure test (MES test), minimal clonic seizure test (6Hz test) and s.c. metrazol seizure threshold test (s.c. MET test) as well as in the rotorod neurotoxicity test (Tox test). One selected compound was tested quant. in 6Hz-test in mice after i.p. administration and showed activity ED50 = 385.69 mg/kg and TD50 > 600 mg/kg (1). In the experiment, the researchers used many compounds, for example, Isoquinoline-1-carboxylic acid (cas: 486-73-7Reference of 486-73-7).

Isoquinoline-1-carboxylic acid (cas: 486-73-7) belongs to isoquinoline derivatives. Although isoquinoline derivatives can be synthesized by several methods, relatively few direct methods deliver the unsubstituted isoquinoline. Lewis acid activation and nucleophilic attack can produce multiple regioisomers in quinolines and pyridines; isoquinolines generally only undergo attack at the 1-position.Reference of 486-73-7

Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem