Macrolides with antitumor activity
AssigneeInstituto Biomar S.A.
InventorsRosa Isabel Fernandez-Chimeno, Francisco Romero, Jose Luis Fernandez-Puentes, Julia Perez-Baz, Librada Maria Canedo, Fernando Espliego
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Abstract
The compound referred to herein as IB-962 12, having structure (I) can be obtained by cultivating the strain of Micromonospora sp. ES25-008, available under the accession number CECT-3333, and can be hydrolyzed to give IB-96212B having structure (II). The sugar substituent which is L-rhodinose, can its elf be derivatized or the sugar can be replaced, in either case, giving further derivatives of IB-96212 having a group other than L-rhodinose at the position of the sugar.
Claims13
A compound of the formula:
- wherein R is hydrogen or a substituent group selected from the group consisting of a mono-, di- or tri-saccharide, C1-6 alky, C2-C7 acyl, cyclo-(C4-C8)-alkyl, phenyl, naphthyl, benzyl and a 4 to 8 membered heterocyclic group having 1 to 4 heteroatoms.
The compound referred to herein as IB-96212, said compound exhibiting spectral characteristics in which:
- FIG. 1 is a HPLC chromatogram of purified IB-96212;
- FIG. 2 is an ultraviolet spectrum (UV) of purified IB-96212;
- FIG. 3 is an infrared (IR) spectrum of purified IB-96212;
- FIG. 4 is a proton NMR (1H) spectrum of purified IB-96212;
- FIG. 5 is a carbon-13 NMR (13C) spectrum of purified B-96212;
- and
- FIG. 6 is a mass spectrum of purified IB-96212.
A process for producing the compound IB-96212, which comprises the step of:
- cultivating a strain of a microorganism capable of producing the compound IB-96212 in an aqueous nutrient medium under controlled conditions,
- wherein the microorganism comprises the culture strain of Micromonospora sp. ES25-008, and
- wherein the cultivation is conducted for sufficient time to form an isolatable quantity of the compound IB-96212.
A process for producing the compound IB-96212B which comprises hydrolysis of the compound IB-96212.
An antitumor pharmaceutical composition comprising the compound IB-96212 or IB-96212B in an amount effective against one or more mammalian tumors and a pharmaceutically acceptable carrier, diluent or excipient.
The biologically pure strain Micromonospora sp. ES25-008, available under the accession number CECT-3333.
Dependencies are inferred from the claim text.