| 摘要 |
Disclosed are compounds of the formula: wherein R1, R2, R3 and R4 are independently hydrogen, C1-C6 alkyl, halo, a sulfate, a glucuronide,—OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl,—N(CH2)n; a phosphate group, and a phosphinate group; R9 is hydrogen, halogen or alkyl; R11 is selected from the group consisting of H, C1-C6 alkyl, halogen, a sulfate, a glucoronide,—SO2NH2,—COOH,—CN,—CH2CN—,—NHCN—,—CHO,═CHOCH3,—COO salt,—OSO2alkyl,—NH2, and—NHCO(CH2)n; R12 is selected from the group consisting of H, a C1-C6 alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X is selected from the group consisting of C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, halogen, a glucoronide,—NH2,—SO2NH2,—COOH,—CN,—CH2CN,—NHCN,—CHO,—COOsalt,—OSO2alkyl,—SH,—SCH3,—CH[(CH2)nCH2]COOCH2,—(CH2)mCOOCH3,—(CH2)m—O—CH3,—(CH2)m—O—(CH2)nCH3, (CH2)m—S—CH3,—(CH2)m—S—(CH2)nCH3,—(CH2)m—NH—(CH2)nCH3,—C2-C8 alkenyl-O—(CH2)nCH3,—C2-C8 alkenyl-S—(CH2)nCH3,—C2-C8 alkenyl-N—(CH2)nCH3,—C2-C8 alkynyl-O—(CH2)nCH3,—C2-C8 alkynyl-S—(CH2)nCH3,—C2-C8 alkynyl-N—(CH2)nCH3,—(CH2)m—OH,—(CH2)m—O—NH2,—(CH2)m—S—NH2,—NH(CH2)mCH3,—NH(CH2)mOCH3,—NH(CH2)mCHOH—COOH,—N(CH3)2,—(CH2)m(NH)CH2OH,—NHCOOH,—(CH2)mNHCOOH,—NO2,—SCN,—SO2alkyl,—B(OH)2,—(CH2)m N(CH3)—SO2—NH3,—(CH2)m—NH—SO2—NH2,—NHC(═S)CH3, and—NHNH2; and Y is selected from hydrogen,═O,—OCO(R6) and—OH; wherein m is an integer between 0-20, n is an integer between 0-8, the symbol represents either a single or a double bond capable of forming a keto group at position 3 or 17; and the symbol represents any type of bond regardless of the stereochemistry; and the respective enantiomers, other stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of said compounds. The compounds are useful in the treatment of various types of cancer.
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