Substrate‐directed Synthesis of Isocoumarin and 3‐Ylidenephthalide Conjugated Noscapinoids and their Antiproliferative Activities.

Autor:	Kumar Pedapati, Ravi, Chirra, Nagaraju, Pranathi Abburi, Naga, Bollikonda, Rakesh, Alekhya, Danaboiena, Sridhar, Balasubramanian, Naik, Pradeep K., Kantevari, Srinivas
Předmět:	COUMARINS ISOCOUMARINS CELL lines CANCER cells RING formation (Chemistry) PHTHALIDES
Zdroj:	Chemistry - An Asian Journal; 1/17/2023, Vol. 18 Issue 2, p1-9, 9p
Abstrakt:	A series of new noscapinoids designed; synthesized and assessed whether its 3‐ylidenephthalide and isocoumarin conjugates improved cytotoxicity. Cu‐catalysed Sonogashira coupling of N‐propargyl noscapine with 2‐bromobenzoic acids followed by in‐situ substrate‐directed 5‐exo‐dig or 6‐endo‐dig cyclization produced 3‐ylidenephthalide 6 a–6 f and isocoumarin 7 a–7 h analogues in very good yields. In comparison to the lead drug, noscapine, all the newly synthesised derivatives exhibited strong cytotoxic potential in vitro with IC50 ranging from 5.4 μM to 39.5 μM across the evaluated panel of cancer cell lines, without harming normal cells (IC50 >300 μM). [ABSTRACT FROM AUTHOR]
Databáze:	Complementary Index
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