Title:
7-ETHYL-10-HYDROXYCAMPTOTHECIN PRODRUG HAVING FLUORESCENCE ACTIVITY, PREPARATION METHOD THEREFOR AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/097854
Kind Code:
A1
Abstract:
A 7-ethyl-10-hydroxycamptothecin prodrug having fluorescence activity, a preparation method therefor and the use thereof are disclosed. The 7-ethyl-10-hydroxycamptothecin prodrug (BDP-SN38) with fluorescence activity is prepared by carrying out condensation on carboxyl of a 4,4'-difluoro-4-bora-3a,4a-diaza-s-indacene dye molecule and hydroxyl in position 10 of 7-ethyl-10-hydroxycamptothecin. The BDP-SN38 has good solubility and stability in most medicinal solvents. Compared with SN38, the BDP-SN38 has equivalent anti-tumor activity and high tumor uptake ability, and can emit strong green fluorescence under visible light excitation, thus making it easy to find residual tumors by means of fluorescence after drug therapy so as to conduct further treatment. The BDP-SN38 has good application prospects in research on integrated diagnosis and treatment and effective tumor treatment.
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Inventors:
GUO ZHENGQING (CN)
HUANG YANGYANG (CN)
JI DANDAN (CN)
XU HAN (CN)
HE HUI (CN)
AI DINGDING (CN)
HUANG YANGYANG (CN)
JI DANDAN (CN)
XU HAN (CN)
HE HUI (CN)
AI DINGDING (CN)
Application Number:
PCT/CN2021/143135
Publication Date:
June 08, 2023
Filing Date:
December 30, 2021
Export Citation:
Assignee:
UNIV SOOCHOW (CN)
International Classes:
C07F5/02; A61K41/00; A61K49/00; A61P35/00
Foreign References:
CN112047952A | 2020-12-08 | |||
CN103755753A | 2014-04-30 | |||
CN112920210A | 2021-06-08 |
Other References:
LIU YANG, PEI QING, CHEN LI, LI ZHENSHENG, XIE ZHIGANG: "Reduction-responsive fluorescence off–on BODIPY–camptothecin conjugates for self-reporting drug release", JOURNAL OF MATERIALS CHEMISTRY. B, ROYAL SOCIETY OF CHEMISTRY, GB, vol. 4, no. 13, 1 January 2016 (2016-01-01), GB , pages 2332 - 2337, XP093070361, ISSN: 2050-750X, DOI: 10.1039/C6TB00009F
Attorney, Agent or Firm:
CENTRAL SOUTH WELL INTELLECTUAL PROPERTY OFFICE (CN)
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