IPC분류정보
| 국가/구분 |
United States(US) Patent
등록
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| 국제특허분류(IPC7판) |
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| 출원번호 |
US-0548060
(1990-07-05)
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발명자
/ 주소 |
- Rinehart Kenneth L. (Urbana IL) Holt Tom G. (Westfield NJ)
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| 출원인 / 주소 |
- Board of Trustees of the University of Illinois (Urbana IL 02)
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| 인용정보 |
피인용 횟수 :
30 인용 특허 :
0 |
초록
▼
The present invention relates to novel compositions of matter extracted from the well-known and readily available tropical marine invertebrate, Ecteinascidia turbinata, and designated herein as ecteinascidins 729, 743, 745, 759A, 759B and 770. These compounds are useful as antibacterial and/or antit
The present invention relates to novel compositions of matter extracted from the well-known and readily available tropical marine invertebrate, Ecteinascidia turbinata, and designated herein as ecteinascidins 729, 743, 745, 759A, 759B and 770. These compounds are useful as antibacterial and/or antitumor agents in mammals.
대표청구항
▼
The substantially pure compound Ecteinascidin 729, free of cellular components of the marine tunicate Ecteinascidia turbinata, said compound having the following physicochemical characteristics: TLC (SiO2) R4-0.28 (3:1 ethyl acetate-methanol), 0.26 (9:1 chloroform-methanol); HPLC retention time, 15.
The substantially pure compound Ecteinascidin 729, free of cellular components of the marine tunicate Ecteinascidia turbinata, said compound having the following physicochemical characteristics: TLC (SiO2) R4-0.28 (3:1 ethyl acetate-methanol), 0.26 (9:1 chloroform-methanol); HPLC retention time, 15.7 min. [Whatman Partisil 10 ODS-3, 10×250 mm, 70:30 methanol-aqueous Tris (0.05M, pH 7.5), 2.8 mL/min.]; UV max (CH3OH), 202 nm (e61 000), 244 (sh) (11 000), 283 (5 000), 289 (4 700), (0.1N HCl) 204 (61 000), 244 (sh) (9 600), 283 (4 800), 289 (4 500), (0.1N KOH) 215 (33 800), 258 (8 200), 290 (6 400); IR (CCl4), 3555, 3535, 2953, 2927, 2855, 1770, 1742, 1504, 1466, 1462, 1454, 1432, 1369, 1239, 1196, 1168, 1122, 1100, 1086, 1054, 1032, 997, 960 cm-1; 1H NMR (360 MHz, CDCl3) e6.63 (s, 1H), 6.48 (s, 1H), 6.44 (s, 1H), 6.04 (d, J-0.7 Hz, 1H), 5.95 (d, J-0.9 Hz, 1H), 5.15 (d, J-10.7 Hz, 1H), 4.84 (bs, 1H), 4.52 (d, J-3.5 Hz, 1H), 4.48 (bs, 1H), 4.38 (d, J-4.9 Hz, 1H), 4.04 (d, J-11 Hz, 1H), 3.78 (s, 3H), 3.62 (s, 3H), 3.61 (m, 2H), 3.10 (m, 1H), 3.02 (d, J-18 Hz, 1H), 2.90 (dd, J-9, 18 Hz, 1H), 2.80 (m, 1H), 2.60 (m, 1H), 2.50 (m, 1H), 2.35 (m, 1 H), 2.31 (s, 3H), 2.27 (s, 3H), 2.20 (m, 1H), 2.03 (s, 3H); FABMS m/z (rel. intensity) 730.2493 (30), 495 (2), 493 (2), 481 (2), 479 (2), 463 (4), 461 (2), 449 (4), 205 (8), 204 (8), 190 (8); B/E linked scan on m/z 729, m/z 711, 696, 683, 509, 495, 481, 479, 461, 449; optical rotation [aD25+112°(c 0.01, CH3OH).
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