| 摘要 |
Described herein are analogues of 2-methyl-3-(2-ethynylthiazol-4-yl)cyclopent-2-enol and the corresponding ketone 3-(2-ethynylthiazol-4-yl)-2-methylcyclopent-2-enone, the analogues having terminal alkyne groups at the 2-position of the thiazole ring. These drug-like molecules, referred to as CETZOLE compounds, are useful to treat non-small cell lung cancer and other forms of cancer. Methods of making and using the compounds, methods of treating various diseases, pharmaceutical compositions, and kits are also disclosed. |
| 主权项 |
1. A compound comprising the following structural formula:wherein:
n=1 or 2; X is N or CH; Y is S, O, or NH; R is ═O; 2H; —OR3, wherein R3 is hydrogen, alkyl, aryl, glycosyl, or polyether groups; (CO)OR4, wherein R4 is hydrogen, alkyl, aryl, or aralkyl groups; —NR5R6, wherein R5 and R6 are H, alkyl, aryl, or aralkyl groups; or ═N—OR7, wherein R7 is hydrogen, alkyl, aryl, aralkyl, glycosyl, or polyether groups; R1 is hydrogen, alkyl-, aryl-, or aralkyl; Z is absent or selected from the group consisting of: halide, wherein R2 is absent; oxygen; nitrogen, wherein there are two R2 groups; (CO)O—; O(CO)—; O(CO)O—; (CO)N<, wherein there are two R2 groups; NH(CO)—; and NH(CO)N<, wherein there are two R2 groups; wherein when Z is absent, R2 connects directly to a ring; and R2 is hydrogen, alkyl-, aryl-, aralkyl-, glycosyl-, or polyether-, wherein multiple occurrences of R2 are the same or different;and prodrugs, salts, stereoisomers, racemates, prodrugs, solvates, and hydrates thereof. |
