Flavone-based dual PARP-Tubulin inhibitor manifesting efficacy against endometrial cancer

Sachin Sharma & Kunal Nepali et al. · 2023-11-02

11Citations
Structural tailoring of the flavone framework (position 7) via organopalladium-catalyzed C-C bond formation was attempted in this study. The impact of substituents with varied electronic effects (phenyl ring, position 2 of the benzopyran scaffold) on the antitumor properties was also assessed. Resultantly, the efforts yielded a furyl arm bearing benzopyran possessing a 4-fluoro phenyl ring (position 2) (
Links
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Journal
Journal of Enzyme Inhibition and Medicinal Chemistry
TL;DR

Structural tailoring of the flavone framework via organopalladium-catalyzed C–C bond formation via organopalladium-catalyzed C–C bond formation yielded a tractable dual PARP-tubulin inhibitor endowed with an impressive activity profile against endometrial cancer.

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Authors
Sachin Sharma, Kavya Chandra, Aliva Naik, Anamika Sharma, Ram Sharma, Amandeep Thakur, Ajmer Singh Grewal, Ashwani K. Dhingra, Arnab Banerjee, Jing Ping Liou, Santosh Kumar Guru, Kunal Nepali
Funding
Ministry of Science and Technology, Taiwan FundingNational Science and Technology Council Grant MOST-111–2320-B-038 –047National Science and Technology Council Grant NSTC-112–2320-B-038–030-Ministry of Science and Technology, Taiwan Grant MOST111-2113-M038-004SERB Grant SRG/2020/002013DBT, GOI Grant BT/INF/22/SP42543/2021