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Discovery of novel conjugates of quinoline and thiazolidinone urea as potential anti-colorectal cancer agent.

ABSTRACT: Based on the obtained SARs, further structural optimisation of compound BC2021-104511-15i was conducted in this investigation, and totally ten novel quinoline derivates were designed, synthesised and optimised for biological activity. Among them, compound 10a displayed significant in vitro anticancer activity against COLO 205 cells with an IC₅₀ value of 0.11 μM which was over 90-fold more potent than that of Regorafenib (IC₅₀>10.0 μM) and Fruquintinib (IC₅₀>10.0 μM). Furthermore, compound 10a exhibited over 90-fold selectivity towards COLO 205 relative to human normal colorectal mucosa epithelial cell FHC cells. Flow cytometry study demonstrated that compound 10a could induce apoptosis in COLO 205 cells, however, it could not induce cell cycle arrest in COLO 205 cells. The results of preliminary kinase profile study showed that compound 10a was a potential HGFR and MST1R dual inhibitor, with IC₅₀ values of 0.11 μM and 0.045 μM, respectively.

SUBMITTER: Xiong L

PROVIDER: S-EPMC9448386 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature

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Discovery of novel conjugates of quinoline and thiazolidinone urea as potential anti-colorectal cancer agent.

Xiong Li L He Huan H Fan Mengmeng M Hu Liping L Wang Fei F Song Xiaomeng X Shi Shengmin S Qi Baohui B

Journal of enzyme inhibition and medicinal chemistry 20221201 1

Based on the obtained SARs, further structural optimisation of compound BC2021-104511-15i was conducted in this investigation, and totally ten novel quinoline derivates were designed, synthesised and optimised for biological activity. Among them, compound 10a displayed significant in vitro anticancer activity against COLO 205 cells with an IC50 value of 0.11 μM which was over 90-fold more potent than that of Regorafenib (IC50>10.0 μM) and Fruquintinib (IC ...[more]

PMID: 36043496

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Dataset Information

Discovery of novel conjugates of quinoline and thiazolidinone urea as potential anti-colorectal cancer agent.

Publications

Discovery of novel conjugates of quinoline and thiazolidinone urea as potential anti-colorectal cancer agent.

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