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US08524740B2 Synthesis and anticancer activity of aryl and heteroaryl-quinolin derivatives 有权
芳基和杂芳基 - 喹啉衍生物的合成和抗癌活性

Synthesis and anticancer activity of aryl and heteroaryl-quinolin derivatives
Abstract:
A compound of Formula I is disclosed as follows: or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R is hydrogen, P(═O)(OH)2, P(═O)(O(C1-C18)alkylene(C6-C20)aryl)2, P(═O)(OH)(OM), P(═O)(OM)2, P═O(O2M), S(═O)(OH)2, S(═O)(O(C1-C18)alkylene(C6-C20)aryl)2, S(═O)(OH)(OM), S(═O)(OM)2; M is a monovalent or divalent metal ion, or alkylammonium ion; W is (C6-C20)aryl, (C6-C20)heteroaryl, (C1-C18)alkyl(C6-C20)aryl, (C1-C18)alkyl(C6-C20)heteroaryl, hydroxy(C6-C20)aryl, hydroxy(C6-C20)heteroaryl, (C1-C18)alkoxy(C6-C20)aryl, (C1-C18)alkoxy(C6-C20)heteroaryl, (C1-C18)alkylenedioxy(C6-C20)aryl, (C1-C18)alkylenedioxy(C6-C20)heteroaryl, halo(C6-C20)aryl, halo(C6-C20)heteroaryl, (C1-C18)alkylamino(C6-C20)aryl, (C1-C18)alkylamino(C6-C20)heteroaryl, (C1-C18)cycloalkylamino(C6-C20)aryl, or (C1-C18)cycloalkylamino(C6-C20)heteroaryl, and their OR8 substutes; R5 is (C1-C18alkoxy, hydrogen, hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, or R5 and R6 are (C1-C18)dioxy provided that R7 is hydrogen; R6 is hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, (C1-C18)alkoxy, (C1-C18)alkylamino, or (C1-C18)cycloalkylamino, or R6 and R7 are (C1-C18)dioxy provided that R5 is hydrogen; R7 is hydrogen, halo or OR8, hydroxyl, or O—(C1-C18)alkyl(C6-C20)aryl; and R8 is P(═O)(OH)2, P(═O)(O(C1-C18)alkyl(C6-C20)aryl)2, P(═O)(OH)(OM), or P(═O)(OM)2, P═O(O2M).
Abstract(Chinese):

式I化合物公开如下：或其药学上可接受的盐，前药，溶剂合物或代谢物，其中R是氢，P（= O）（OH）2，P（= O）（O（C 1 -C 18） ）亚烷基（C 6 -C 20）芳基）2，P（= O）（OH）（OM），P（= O）（OM）2，P = O（O 2 M） S（= O）（O（C1-C18）亚烷基（C6-C20）芳基）2，S（= O）（OH）（OM），S（= O）（OM） M是一价或二价金属离子或烷基铵离子; W是（C 6 -C 20）芳基，（C 6 -C 20）杂芳基，（C 1 -C 18）烷基（C 6 -C 20）芳基，（C 1 -C 18）烷基（C 6 -C 20） 羟基（C 6 -C 20）杂芳基，（C 1 -C 18）烷氧基（C 6 -C 20）芳基，（C 1 -C 18）烷氧基（C 6 -C 20）杂芳基，（C 1 -C 18）亚烷基二氧基 C 1 -C 20烷基氨基（C 6 -C 20）芳基，（C 1 -C 20）芳基，（C 1 -C 20）芳基， 杂芳基，（C1-C18）环烷基氨基（C6-C20）芳基或（C1-C18）环烷基氨基（C6-C20）杂芳基及其OR8分子; R5是（C1-C18烷氧基，氢，羟基，O-（C1-C18）烷基（C6-C20）芳基，卤素或OR8或R5和R6是（C1-C18）二氧基，条件是R7是氢; R6是羟基 ，（C 1 -C 18）烷基（C 6 -C 20）芳基，卤素或OR 8，（C 1 -C 18）烷氧基，（C 1 -C 18）烷基氨基或（C 1 -C 18）环烷基氨基或R 6和R 7为 （C 1 -C 18）烷基（C 6 -C 20）芳基; R 8为P（= O）（OH）2，P（= O） = O）（O（C 1 -C 18）烷基（C 6 -C 20）芳基）2，P（= O）（OH）（OM）或P（= O）（OM）2，P = O（O 2 M）。

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