2(3)-methylthio styryl benzofuran quinolone derivative, and preparation method and application thereof

• Main Authors: ZHANG QI, PENG WANG, SUN ZHIYIN, OU TIANMIAO, WANG SHIKE, HUANG ZHISHU
• Format: Patent
• Language: Chinese; English
• Published: 14.09.2018
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention relates to a 2(3)-methylthio styrylbenzofuran quinolone derivative, and a preparation method and application thereof. The structural formula of the derivative is shown as the formula (1)or the formula (2), wherein R refers to C2-3 alkyldiamine, N-methyl substituted C2-3 alkyldiamine, 4-N substituted piperazinyl, terminal substituted C1-3 alkylamido or morpholinyl, and X refers to Oor N. Methylthiostyrene is introduced onto A rings of indoloquinoline, benzofuran quinolone, 5-N-methylated indoloquinoline, and parent skeletons of parent skeleton compounds of 5-N-methylated benzofuran quinolone compounds, different amino side chains are introduced to 11 sites to interact with NRAS RNA G-quadruplex, and accordingly, the 2(3)-methylthio styrylbenzofuran quinolone derivative has high selectivity and activity, low toxicity and good antitumor effect. 本发明涉及种2（3）-对甲硫基苯乙烯基苯并呋喃喹啉衍生物及其制备方法和应用。所述衍生物的结构式如式（Ⅰ）或式（Ⅱ）所示：其中，R为C2~3烷二胺基、N-甲基取代C2~3烷二胺基、4-N取代哌嗪基、末端取代C1~3烷胺基或吗啉基；X为O或N。在吲哚并喹啉，苯并呋喃喹啉，5-N-甲基化吲哚并喹啉，以及5-N-甲基化