ChemInform Abstract: Medicinal Chemistry and Chemical Biology of Diketopiperazine-Type Antimicrotubule and Vascular-Disrupting Agents

ChemInform ◽  
2013 ◽  
Vol 45 (1) ◽  
pp. no-no
Author(s):  
Yoshio Hayashi ◽  
Yuri Yamazaki-Nakamura ◽  
Fumika Yakushiji
Keyword(s):  
Chemical Biology ◽  
Medicinal Chemistry ◽  
Vascular Disrupting Agents ◽  
Vascular Disrupting

scholarly journals Synthesis and Cytotoxic Activity of Several Novel N-Alkyl-Plinabulin Derivatives With Aryl Group Moieties

2021 ◽  
Vol 16 (4) ◽  
pp. 1934578X2110100
Author(s):  
Pham The Chinh ◽  
Pham Thi Tham ◽  
Duong Huong Quynh ◽  
Nguyen Van Tuyen ◽  
Dinh Thuy Van ◽  
...  
Keyword(s):  
Cytotoxic Activity ◽  
Cancer Cells ◽  
Cell Lines ◽  
Cancer Cell ◽  
Aldol Condensation ◽  
One Pot ◽  
Aryl Group ◽  
Vascular Disrupting Agents ◽  
Benzaldehyde Derivatives ◽  
Vascular Disrupting

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.

scholarly journals Medicinal Chemistry and Chemical Biology of New Generation Taxane Antitumor Agents

IUBMB Life ◽  
2002 ◽  
Vol 53 (4-5) ◽  
pp. 269-274 ◽  
Author(s):  
Iwao Ojima ◽  
Raphaël Geney ◽  
Ioana Maria Ungureanu ◽  
Dansu Li
Keyword(s):  
Chemical Biology ◽  
Medicinal Chemistry ◽  
Antitumor Agents ◽  
New Generation

scholarly journals Current Innovations in Medicinal Chemistry and Chemical Biology

2018 ◽  
Vol 9 (6) ◽  
pp. 513-514 ◽  
Author(s):  
Stevan W. Djuric ◽  
Anil Vasudevan
Keyword(s):  
Chemical Biology ◽  
Medicinal Chemistry
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