We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Synthesis and Cytotoxic Activity of Several Novel N-Alkyl-Plinabulin Derivatives With Aryl Group Moieties.
- Authors
Pham The Chinh; Pham Thi Tham; Duong Huong Quynh; Nguyen Van Tuyen; Dinh Thuy Van; Phan Thanh Phuong; Tran Thi Thu Hang; Phan Van Kiem
- Abstract
Seven novel N-alkyl-plinabulin derivatives with aryl groups moieties (nitroquinoline, 1,4-dihydroquinoline, 4-methoxybenzene, and 4-chlorobenzene) have been synthesized via aldol condensation and alkylation in one-pot, and tested for their cytotoxicity against 4 cancer cell lines (KB, HepG2, Lu, and MCF7). Compounds (Z)-3-((6,8-dimethyl-4-oxo-1,4-dihydroquinolin-2-yl) methylene)-6-((Z)-4-methoxybenzylidene)-1-(prop-2-yn-1-yl) piperazine-2,5-dione (5a), (Z)-6-((Z)-4-methoxybenzylidene)-1-(prop-2-yn-1-yl)-3-((1,6,8-trimethyl-4-oxo-1,4-dihydroquinolin-2-yl) methylene)piperazine-2,5-dione (5b), and (Z)-3-((Z)-4-chlorobenzylidene)-1,4-dimethyl-6-((8-methyl-4-nitroquinolin-2-yl) methylene)piperazine-2,5-dione (8) showed strong cytotoxicity against 3 of the cancer cells lines (KB, HepG2 and Lu) with IC50 values ranging from 3.04 to 10.62 µM. The quinoline-derived compounds had higher cytotoxic activity than the benzaldehyde derivatives. The successful synthesis of these derivatives offers useful information for the development of more potent vascular disrupting agents based on plinabulin.
- Subjects
ARYL group; MOIETIES (Chemistry); NITROQUINOLINE oxide; ANISOLE; ALKYLATION
- Publication
Natural Product Communications, 2021, Vol 16, Issue 4, p1
- ISSN
1934-578X
- Publication type
Article
- DOI
10.1177/1934578X211010040