主权项 |
1. A compound of formula I:or a pharmaceutically acceptable salt thereof;wherein:
each independently designates a single or double bond; R1 is hydrogen, optionally substituted C1-6 aliphatic, —(CH2)nCO2R8, —(CH2)nCON(R8)2, —(CH2)nCOSR8, or taken together with R2 to form an optionally substituted, saturated or unsaturated 3-7-membered ring having 0-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; and each R8 is independently hydrogen, an optionally substituted group selected from cephalotaxine, C1-6 aliphatic, 6-10-membered aryl, or C1-6 heteroaliphatic having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur;n is an integer from 0-4;
R2 is hydrogen, —NR2, —OR, or an optionally substituted group selected from acyl, C1-6 aliphatic, or C1-6 heteroaliphatic having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R3 is -T-Rz, wherein: T is a covalent bond or a bivalent C1-12 saturated or unsaturated, straight or branched, hydrocarbon chain, wherein one or two methylene units of T are optionally and independently replaced by —O—, —S—, —N(R)—, —C(O)—, —C(O)O—, —OC(O)—,—N(R)C(O)—, —C(O)N(R)—, —S(O), —S(O)2—, —N(R)SO2—, or —SO2N(R)—; and
Rz is hydrogen, halogen, a monosaccharide, a disaccharide, —OR, —SR, —NR2, —N3, or an optionally substituted group selected from acyl, arylalkyl, heteroarylalkyl, C1-6 aliphatic, 6-10-membered aryl, 5-10-membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, 4-7-membered heterocyclyl having 1-2 heteroatoms independently selected from nitrogen, oxygen or sulfur; or a hydrogen radical on Rz is replaced with a substituent of the formula: wherein each occurrence of R1, R2, R4, R5, R6, R7, T, and Rz may be the same or different; R4 is hydrogen, —OR, or ═O; R5 and R6 are each independently selected from hydrogen, C1-6 aliphatic, —SO2R, —CO2R; or R5 and R6 are taken together with their intervening atoms to form an optionally substituted 5-7-membered ring having 0-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R7 is hydrogen, —OR, —OCO2R, —OCOR, —OCOSR, or —OCONR2; and each R is independently hydrogen, an optionally substituted group selected from acyl, arylalkyl, C1-6 aliphatic, or C1-6 heteroaliphatic having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or two R on the same nitrogen atom are taken with the nitrogen to form a 4-7-membered heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, or sulfur; with the proviso that at least one of R5, R6, or R7 is not hydrogen.
|