Synthesis and biological evaluation of cytogenin derivatives.
To enhance the stability in vivo, new derivatives of cytogenin were synthesized, and their biological activity and stability in mice were estimated. 2-(8-Hydroxy-6-methoxy-1-oxo-1H-2-benzopyran-3-yl)propionic acid (NM-3) was found to be the most stable among them. It modified collagen-induced arthritis in mice. It also showed potent anti-angiogenic activity in a mouse dorsal air sac assay.
Matsumoto
N
N
Central Research Laboratories, Mercian Corp, Johnan, Fujisawa, Japan. n-matsumoto@hkg.odn.ne.jp
Nakashima
T
T
Isshiki
K
K
Kuboki
H
H
Hirano
S I
SI
Kumagai
H
H
Yoshioka
T
T
Ishizuka
M
M
Takeuchi
T
T
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D000903:Antibiotics, Antineoplastic / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001168:Arthritis / Q000188:drug therapy; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D004355:Drug Stability; D066298:In Vitro Techniques; D049934:Isocoumarins; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D008811:Mice, Inbred DBA; D008813:Mice, Inbred ICR; D009389:Neovascularization, Pathologic / Q000188:drug therapy; D051381:Rats; D017207:Rats, Sprague-Dawley; D013056:Spectrophotometry, Ultraviolet; D017550:Spectroscopy, Fourier Transform Infrared
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000903:Antibiotics, Antineoplastic; D003374:Coumarins; D049934:Isocoumarins; C453300:isocoumarin NM-3; C066806:cytogenin