Title:Design, Synthesis, Characterisation, and Evaluation of Substituted
Quinolin-2-one Derivatives as Possible Anti-lung Cancer Agents
Volume: 21
Issue: 4
Author(s): Riya Swar, Prachita Gauns Dessai*, Shivalingrao MamleDesai, Sachin Chandavarkar, Soniya Phadte and Bheemanagouda Biradar
Affiliation:
- Department of Pharmaceutical Chemistry, PES’s Rajaram and Tarabai Bandekar College of Pharmacy, Ponda, Goa
403 401, India
Keywords:
Quinolin-2-one, anticancer, molecular docking, lung cancer, ADMET profile, breast cancer.
Abstract:
Background: According to 2022, the estimated number of cancer cases in India was found
to be 1,461,427. Lung cancers are the leading cause of death among Indian males. Research on cancer
has been conducted to develop better treatments that are safe and effective and could be used to diagnose
cancer at an early stage. It was found that quinolin-2-one possesses anticancer activity, which
led us to synthesize substituted quinolin-2-one derivatives that can provide a longer future to cancer
patients and decrease the risk of dying from cancer.
Objective: This study aimed to carry out the design, synthesis, characterisation, and evaluation of
novel substituted quinolin-2-one analogues as possible anti-lung cancer agents.
Methods: Compound III a/III b on reaction with acids, sodium acetate and ethylchloroacetate, substituted
benzaldehyde, phthalic anhydride, and 2N sodium hydroxide yielded compounds IV a/ IV b,
V a/ V b, VI a/ VI b, VI c/ VI d, VI e/ VI f, VII a/ VII b, and VIII a/ VIII b, respectively.
Result: Among all the synthesised derivatives, compound VII a was found to be most potent with a
MolDock score of -132.78 as compared to standard drug imatinib (-114.37) and active ligand 4- anilinoquinazoline
(-126.71). All the synthesized derivatives showed a good ADME profile, but compound
VII a showed the best ADME data among all the synthesised derivatives.
All the synthesised compounds were tested for their in vitro anticancer activity against the Hop-62
(human lung cancer) cell line, out of which compound VII a was found to be most potent, with a
percent control growth of -51.7% at a concentration of 80 μg/ml, which was in comparable to the
positive control, Adriamycin (-70.5%) and standard imatinib (-84.0%).
Conclusion: Compound VII a showed the highest MolDock score and was most potent against human
lung cancer cell line Hop-62.
