Synthesis and antitumor activity of a series of lactone-opened camptothecin derivatives.

A series of E-ring lactone-opened camptothecin (CPT) derivatives bearing with terminal aza-heterocyclic groups were synthesized, and their antitumor activity was evaluated both in vitro and in vivo. Hydroxyl-amide analogues with morpholin-4-yl displayed excellent antitumor activity in vitro and efficient inhibition on tumor xenograph model in nude mice. Ester-amide compounds acted less active in vitro cytotoxicity and lower inhibition activity in vivo. Substitutions at 7- and 10- positions favored the antitumor activity.

[3,3'-Dihy-droxy-3,3'-bis-(pyridin-3-yl-κN)-1,1'-(pyridine-2,6-di-yl)dipropan-1-one](nitrato-κO,O')silver(I).

In the title compound, a new macrocyclic metal complex, [Ag(NO(3))(C(21)H(15)N(3)O(4))], all non-H atoms are in a close-to-planar geometry (except for the nitrate anion), with a maximum out-of-plane deviation of 0.327 (6) Šfor a pyridine C atom. The dihedral angle between the least-squares plane through the [3,3'-dihy-droxy-3,3'-bis-(pyridin-3-yl)-1,1'-(pyridine-2,6-di-yl)dipropan-1-one]silver(I) fragment and the nitrate anion is 31.29 (13)°. The mol-ecular structure is stabilized by several inter- and intra-molecular O-H⋯O and C-H⋯O hydrogen bonds. The Ag(I) atom is coordinated by two pyridine N atoms and two O atoms of the nitrate anion in a geometry intermediate between tetrahedral and square-planar.

3-(2-Bromo-benz-yl)-1-methyl-1H-imidazol-3-ium bromide.

In the title compound, C(11)H(12)BrN(2) (+)·Br(-), the imidazole and phenyl rings are nearly perpendicular, making a dihedral angle of 87.71 (7)°. The crystal structure is stabilized by non-classical inter-molecular C-H⋯Br hydrogen bonds and inversion-related mol-ecules are linked through π-π inter-actions between the imidazole ring systems [centroid-centroid distance = 3.472 (6) Å].

2,6-Bis(3-phenyl-1H-pyrazol-5-yl)pyridine monohydrate.

In the title compound, C(23)H(17)N(5)·H(2)O, the pyrazole rings are slightly twisted from the central pyridine ring, forming dihedral angles of 5.3 (2) and 3.5 (2)°. The pyrazole and phenyl rings on each side of the pyridine ring are also approximately coplanar, making dihedral angles of 6.0 (2) and 4.5 (2)°. In the crystal structure, 2,6-bis-(3-phenyl-1H-pyrazol-5-yl)pyridine and water mol-ecules are linked together via N-H⋯O and O-H⋯N hydrogen bonds, forming a column running parallel to the a axis.