Karthikeyan Chandrabose, Amawi Haneen, Ashby Charles R, Khare Vishwa M, Jones Veronica, Hari Narayana Moorthy N S, Trivedi Piyush, Tiwari Amit K
Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak, 484887, India.
School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Bhopal, 462036, India.
Heliyon. 2019 May 14;5(5):e01603. doi: 10.1016/j.heliyon.2019.e01603. eCollection 2019 May.
A novel series of 3-((2-chloroquinolin-3-yl)methylene)indolin-2-ones were synthesized, using the 'molecular hybridization approach' and evaluated for anticancer efficacy. Eleven 3-((2-chloroquinolin-3-yl)methylene)indolin-2-ones ( to ) were synthesized and evaluated for cytotoxic efficacy in cancer (ovarian, prostate and colon) and two non-cancerous cell lines. Among the 3-((2-chloroquinolin-3-yl)methylene)indolin-2-one derivatives, with a 6-Cl substitution in the 3-quinolinyl moiety, had selective and potent cytotoxic efficacy in the ovarian cancer cell line A2780. Further mechanistic investigations indicated that significantly inhibited the clonogenic survival of A2780 cancer cells, which was mediated by inducing apoptosis.
采用“分子杂交方法”合成了一系列新型的3-((2-氯喹啉-3-基)亚甲基)吲哚啉-2-酮，并对其抗癌疗效进行了评估。合成了11种3-((2-氯喹啉-3-基)亚甲基)吲哚啉-2-酮（至），并在癌症（卵巢癌、前列腺癌和结肠癌）和两种非癌细胞系中评估了其细胞毒性疗效。在3-((2-氯喹啉-3-基)亚甲基)吲哚啉-2-酮衍生物中，在3-喹啉基部分具有6-氯取代的化合物，在卵巢癌细胞系A2780中具有选择性和强效的细胞毒性疗效。进一步的机制研究表明，该化合物显著抑制了A2780癌细胞的克隆存活，这是由诱导凋亡介导的。
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