Synthesis and biological evaluation against of novel hybrid molecules containing indazole-based 2-pyrone scaffolds.

A series of novel indazole-pyrone hybrids were synthesized by a one pot reaction between -alkyl-6(5)-nitroindazoles and 2-pyrone (4-hydroxy-6-methyl-2-pyran-2-one) using indium or stannous chloride as the reducing system in the presence of acetic acid in tetrahydrofuran. The hybrid molecules were obtained in good to excellent yields (72-92%) and characterized by NMR and single crystal X-ray diffraction. Nineteen compounds were tested against both (MHOM/ET/67/HU3, also called LV9) axenic and intramacrophage amastigotes.

Crystal structure of (Z)-3-allyl-5-(4-chloro-benzyl-idene)-2-sulfanyl-idene-1,3-thia-zolidin-4-one.

In the title compound, C13H10ClNOS2, the dihedral angle between the rhodanine (r.m.s.

Crystal structure of (E)-3-allyl-2-sulfanyl-idene-5-[(thio-phen-2-yl)methyl-idene]thia-zolidin-4-one.

Mol-ecules of the title compound, C11H9NOS3, are built up by one thio-phene and one 2-thioxa-thia-zolidin-4-one ring which are connected by a methyl-ene bridge. In addition, there is an allyl substituent attached to nitro-gen. The two rings are almost coplanar, making a dihedral angle between them of 0.

Synthesis and in-vitro cytotoxic evaluation of novel pyridazin-4-one derivatives.

A new series of N-aryl-4-oxo-1,4-dihydro-pyridazine-3-carboxylic acids has been synthesized by condensation of aryldiazonium with 4-hydroxy-6-methyl-2-pyrone. Some of these compounds exhibited in-vitro cytotoxic activity with moderate to excellent growth inhibition against the murine P815 mastocytoma cell line. Compound 5b showed an important cytotoxic activity against cell line P815 (IC(50 )= 0.