NOVEL VITAMIN D ANALOGS AS ANTI-CANCER DRUGS

Award Information
Agency: Department of Health and Human Services
Branch: N/A
Contract: N/A
Agency Tracking Number: 19107
Amount: $50,000.00
Phase: Phase I
Program: SBIR
Awards Year: 1992
Solicitation Year: N/A
Solicitation Topic Code: N/A
Solicitation Number: N/A
Small Business Information
Steroids Ltd
2201 West Campbell Park Drive, Chicago, IL, 60612
DUNS: N/A
HUBZone Owned: N
Woman Owned: N
Socially and Economically Disadvantaged: N
Principal Investigator
 Raju Penmasta
 (312) 421-1819
Business Contact
Phone: () -
Research Institution
N/A
Abstract
SIDE-CHAIN MODIFIED ANALOGS OF 1 ALPHA, 25-DIHYDROXYVITAMIN D3 HAVE BEEN SHOWN TO SUPPRESS PROLIFERATION OF BONE MARROW MYELOID CELLS AS WELL AS OTHER LEUKEMIA CELL LINES, AND EFECT DIFFERENTIATION BOTH IN VITRO AND IN VIVO OF MYELOID CELLS. THESE PHENOMENA COUPLED WITH LOW CALCEMIC ACTIVITY OFFER PROMISE FOR AN ANTI-CANCER DRUG WHICH MAY BLOCK PROLIFERATION OR CAUSE DIFFERENTIATION OF MYELOID CELLS INTO BENIGN MONOCYTES. WE WILL SYNTHESIZE FOUR NOVEL SIDE-CHAIN ANALOGS OF VITAMIN D2, NAMELY, IN THE C20-NORMAL SERIES: LALPHA-HYDROXY-24-EPI-23-OXAVITAMIN D4, AND PHA-HYDROXY-20-ISO-23-OXA-VITAMIN D4; AND IN THE C20 ISO SERIES: LALPHA-HYDROXY-24-EPI-20-ISO-23-OXAVITAMIN D4 AND LALPHA-HYDROXY-20-ISO-23-OXA-VITAMIN D4. THE RATIONALE FOR SELECTION OF THESE COMPOUNDS IS BASED UPON ANALOGY WITH STRUCTURALLY RELATED C22-OXA ANALOGS WHICH SHOW LOW CALCEMIC ACTIVITY AND GOOD POTENCY IN INDUCTION OF DIFFERENTIATION OF HL-60 LINES. FURTHERMORE, A GENERAL TREND OF SAR INDICATES THAT THE COMPOUNDS WILL BE DEVOID OF CALCEMIC EFFECTS. THESE ANALOGS WILL BE ASSESSED IN AN HL-60 CELL LINE ASSAY, A MOUSE MAMMARY TUMOR SCREEN AND A CALCIUM MOBILIZATION SCREEN.

* information listed above is at the time of submission.

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