Novel 3-((2-chloroquinolin-3-yl)methylene)indolin-2-one derivatives produce anticancer efficacy in ovarian cancer in vitro
Chandrabose Karthikeyan,
Haneen Amawi,
Charles R. Ashby, Jr.,
Vishwa M. Khare,
Veronica Jones,
N.S. Hari Narayana Moorthy,
Piyush Trivedi,
Amit K. Tiwari
Affiliations
Chandrabose Karthikeyan
Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak, 484887, India; School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Bhopal, 462036, India; Corresponding author.
Haneen Amawi
Department of Pharmacology and Experimental Therapeutics, College of Pharmacy & Pharmaceutical Sciences, University of Toledo, OH, USA; Department of Pharmacy Practice, Yarmouk University, Irbid, 21163, Jordan
Charles R. Ashby, Jr.
Department of Pharmaceutical Sciences, St. John's University, Queens, USA
Vishwa M. Khare
Cell and Developmental Biology, School of Medicine, University of Pennsylvania, Philadelphia, PA, USA
Veronica Jones
Department of Biomedical Sciences, Tuskegee University, Tuskegee, AL, USA
N.S. Hari Narayana Moorthy
Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak, 484887, India
Piyush Trivedi
School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Bhopal, 462036, India; Center of Innovation and Translational Research, Poona College of Pharmacy, Bharati Vidyapeeth Deemed University, Pune, India
Amit K. Tiwari
Department of Pharmacology and Experimental Therapeutics, College of Pharmacy & Pharmaceutical Sciences, University of Toledo, OH, USA; Department of Biomedical Sciences, Tuskegee University, Tuskegee, AL, USA; Corresponding author.
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 (LM01 to LM11) were synthesized and evaluated for in vitro 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, LM08, 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 LM08 significantly inhibited the clonogenic survival of A2780 cancer cells, which was mediated by inducing apoptosis.
