ChemInform Abstract: Novel Combretastatin Analogues Effective Against Murine Solid Tumors: Design and Structure—Activity Relationships.
✍ Scribed by K. OHSUMI; R. NAKAGAWA; Y. FUKUDA; T. HATANAKA; Y. MORINAGA; Y. NIHEI; K. OHISHI; Y. SUGA; Y. AKIYAMA; T. TSUJI
- Publisher
- John Wiley and Sons
- Year
- 2010
- Weight
- 36 KB
- Volume
- 29
- Category
- Article
- ISSN
- 0931-7597
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✦ Synopsis
Novel Combretastatin Analogues Effective Against Murine Solid Tumors: Design and Structure-Activity Relationships.
-A series of combretastatin A-4 analogues, e.g. (V) and (VIII), with cis orientation of the two benzene rings and 3,4,5-trimethoxy substituents as indispensable criteria for potent cytotoxicity is synthesized as described. With 2-methoxy-5pyridinecarboxaldehyde as mimic of 3-amino-4-methoxybenzene, isomerization of the obtained trans-stilbene to the required cis-stilbene by means of irradiation is not possible. Compounds (Va), (VIIIb), and, especially, (VIIIa) (all isolated as hydrochlorides) show potent antitumor activity. Further evaluation of (VIIIa) as potential anticancer agent for solid tumors is underway. -(OHSUMI, K.;