新型强效类视黄醇——羧基苯基喹啉及相关化合物的合成与生物活性。视黄酸苯甲酸。VII。
Synthesis and biological activity of carboxyphenylquinolines and related compounds as new potent retinoids. Retinobenzoic acids. VII.
作者信息
Eyrolles L, Kawachi E, Kagechika H, Hashimoto Y, Shudo K
机构信息
Faculty of Pharmaceutical Sciences, University of Tokyo, Japan.
出版信息
Chem Pharm Bull (Tokyo). 1994 Dec;42(12):2575-81. doi: 10.1248/cpb.42.2575.
A series of new quinoline, quinolone, and quinazolinedione derivatives was synthesized and tested for retinoid activity in the human promyelocytic cell line HL-60 differentiation assay. All the quinoline compounds exhibited significant activity, depending on the substituent on the heterocycle. However, the quinolone and quinazolinedione derivatives were poor inducers of the differentiation of the HL-60 cells, the activity depending strongly on the polarity of the molecule.
合成了一系列新的喹啉、喹诺酮和喹唑啉二酮衍生物，并在人早幼粒细胞系HL-60分化试验中测试其类视黄醇活性。所有喹啉化合物均表现出显著活性，这取决于杂环上的取代基。然而，喹诺酮和喹唑啉二酮衍生物对HL-60细胞分化的诱导作用较差，其活性在很大程度上取决于分子的极性。
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