Tropolones are promising organic compounds that can have important biologic effects. We developed a series of new 2-quinolyl-1,3-tropolones derivatives that were prepared by the acid-catalyzed reaction of 4,7-dichloro-2-methylquinolines with 1,2-benzoquinones. 2-Quinolyl-1,3-tropolones have been synthesized and tested for their anti-proliferative activity against several human cancer cell lines. Two compounds (3d and mixture B of 3i–k) showed excellent activity against six cancer cell lines of different tissue of origin. The promising compounds 3d and mixture B of 3i–k also demonstrated induction of apoptotic cell death of ovarian cancer (OVCAR-3, OVCAR-8) and colon cancer (HCT 116) cell lines and affected ERK signaling. In summary, 2-quinolyl-1,3-tropolones are promising compounds for development of effective anticancer agents.

中文翻译：

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2-quinolyl-1,3-tropolone 衍生物作为新型抗癌剂的设计、合成和生物学评价

托酚酮是有前途的有机化合物，具有重要的生物学作用。我们开发了一系列新的 2-quinolyl-1,3-tropolones 衍生物，这些衍生物是通过 4,7-二氯-2-甲基喹啉与 1,2-苯醌的酸催化反应制备的。已经合成了 2-Quinolyl-1,3-tropolones，并测试了它们对几种人类癌细胞系的抗增殖活性。两种化合物（3d和3i-k的混合物 B ）对六种不同来源组织的癌细胞系表现出优异的活性。有前途的化合物3d和3i-k的混合物 B还证明诱导卵巢癌（OVCAR-3，OVCAR-8）和结肠癌（HCT 116）细胞系的凋亡细胞死亡并影响ERK信号传导。总之，2-quinolyl-1,3-tropolone 是用于开发有效抗癌剂的有前景的化合物。