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Current Organic Synthesis

Author(s): Zurong Song*, Qin Lu, Ali Tao and Tianchen Wu

DOI: 10.2174/1570179418666210303113406

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Synthesis and Anti-cancer Activity of Paclitaxel−Coumarin Conjugate

Page: [587 - 591] Pages: 5

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Abstract

Background: Paclitaxel, a natural diterpenoid compound, has anti-tumor effect by acting on tubulin, whereas coumarin, another kind of natural product, has anti-tumor effect, along with some other effects, such as anti-bacterial-., Moreover, it also possesses fluorescence.

Objective: Multi targeting is an effective strategy in drug design to combat tumor. Therefore, a combination of paclitaxel with other active molecular drugs for exploring the novel lead with multi-functions is in demand.

Materials and Methods: To synthsize paclitaxel-coumarin conjugate via click chemistry and to investigate anticancer activity by MTT assay and the scratch test.

Results and Discussion: The results of MTT assay showed that compared tothe paclitaxel, the anti-tumor activity of the conjugate was significantly improved. The results of flow cytometry showed that the conjugate had a stronger ability to induce apoptosis. The scratch test results showed that the conjugate had better anti- metastasis ability than paclitaxel.

Conclusion: These findings indicated that paclitaxel and coumarin had a synergistic effect, which paved the way for the development of paclitaxel through fluorescence.

Keywords: Paclitaxel, coumarin, conjugate, synthesis, anti-tumor activity, anti-metastasis.

Graphical Abstract

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