Gusakov Evgeniy A, Topchu Iuliia A, Mazitova Aleksandra M, Dorogan Igor V, Bulatov Emil R, Serebriiskii Ilya G, Abramova Zinaida I, Tupaeva Inna O, Demidov Oleg P, Toan Duong Ngoc, Lam Tran Dai, Bang Duong Nghia, Boumber Yanis A, Sayapin Yurii A, Minkin Vladimir I
Institute of Physical and Organic Chemistry, Southern Federal University, Rostov-on-Don, 344090, Russia.
Kazan Federal University, Kazan, 420008, Russia.
RSC Adv. 2021;11(8):4555-4571. doi: 10.1039/d0ra10610k. Epub 2021 Jan 22.
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 ( and mixture B of ) showed excellent activity against six cancer cell lines of different tissue of origin. The promising compounds and mixture B of 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.
卓酚酮是一类具有重要生物学效应的有前景的有机化合物。我们开发了一系列新的2-喹啉基-1,3-卓酚酮衍生物，它们是通过4,7-二氯-2-甲基喹啉与1,2-苯醌的酸催化反应制备而成的。2-喹啉基-1,3-卓酚酮已被合成，并针对几种人类癌细胞系测试了其抗增殖活性。两种化合物（以及的混合物B）对六种不同组织来源的癌细胞系表现出优异的活性。有前景的化合物以及的混合物B还证明可诱导卵巢癌（OVCAR-3、OVCAR-8）和结肠癌细胞系（HCT 116）发生凋亡性细胞死亡，并影响ERK信号传导。总之，2-喹啉基-1,3-卓酚酮是开发有效抗癌药物的有前景的化合物。
