Compound containing indoleacetic acid core structure and use thereof
Disclosed are a compound as shown by the following formula 1, and a pharmaceutically acceptable salt, an ester, a hydrate and an organic solvate thereof. In the formula (1), the groups R 1 to R 17 are independently selected from the group consisting of hydrogen, fluorine, chlorine, bromine, iodine, C 1 -C 8 alkyl, C 1 -C 8 alkoxy, carbonyl, hydroxyl, amino, azido, carboxyl and C 1 -C 8 alkylsulfinyl, respectively; and X is a carbon or nitrogen atom; Y is selected from the following groups: a single bond, C 1 -C 8 alkylene, C 6 -C 20 arylene and C 4 -C 20 heteroarylene; and n is an integer from 5 to 20. Also provided in the present invention are a pharmaceutical composition containing the compound, and use thereof in the field of tumor therapy.
1. A compound as shown by formula 1:
wherein, the groups R 1 to R 17 are each independently selected from the group consisting of hydrogen, fluorine, chlorine, bromine, iodine, C 1 -C 8 alkyl, C 1 -C 8 alkoxy, oxo(═O), carbonyl, hydroxyl, amino, azido, carboxyl and C 1 -C 8 alkylsulfinyl; X is a nitrogen atom; Y is selected from the group consisting of single bond, C 1 -C 8 alkylene, C 6 -C 20 arylene and C 4 -C 20 heteroarylene; and n is an integer from 5 to 20, and a pharmaceutically acceptable salt thereof.
2. The compound according to claim 1 , characterized in that the groups R 1 to R 4 are each independently selected from the group consisting of hydrogen, fluorine, chlorine, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, carbonyl, oxo(═O), and hydroxyl; R 11 is selected from the group consisting of hydrogen, fluorine, chlorine, bromine, iodine, azido and C 1 -C 3 alkylsulfinyl; R 6 to R 9 are each independently selected from hydrogen, C 1 -C 4 alkyl and C 1 -C 4 alkoxy; R 5 , R 10 , R 12 to R 17 are each independently selected from hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy and amino; X is a nitrogen atom; Y is selected from the group consisting of single bond, C 1 -C 6 alkylene, C 6 -C 15 arylene and C 4 -C 15 heteroarylene; and n is an integer of 5 to 20.
3. The compound according to claim 1 , characterized in that the compound is selected from the compounds shown by any of the following formulae a, b, e and f, and pharmaceutically acceptable salts thereof:
4. A pharmaceutical composition, comprising:
(i) the compound according to claim 1 or a pharmaceutically acceptable salt prodrug thereof;
(ii) optionally one or more of pharmaceutically acceptable fillers, carriers and diluents; and
(iii) optionally a pharmaceutically active component different from the component (i) selected from one or more of the following substances: uramastine, amifostine, chlorambucil, mustine, cyclophosphamide, paclitaxel, Thiotepa, cisplatin, busulfan, doxorubicin, carmustine 5-fluorouracil, celecoxib, mercaptopurine, methotrexate, tegafur, gefitinib, hydroxyurea, cytosine arabinoside, carboplatin, Iproplatin, prednisone, prednisolone, dexamethasone, diethylstilbestrol, estradiol, raloxifene, Testosterone propionate, semustine, lomustine, thioguanine, etoposide, vincristine, ifosfamide, Navelbine, gemcitabine, mitomycin and vindesine.