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2001 alkaloids alkaloids U 0600 17 - 210 Studies Directed Towards the Refinement of the Pancratistatin Cytotoxic Pharmacophore. The preparation of the deoxy-analogue (VIIIb) of the anticancer/antiviral agent pancratistatin (VIIIa) containing func- tionality complementary to the minimum structural pharmacophore utilizing a Diels–Alder approach is described. Initial anticancer screening of the two deoxy- analogues (VIIIb) and (VIIIc) shows marginal activity for (VIIIc) and selective inhibition of certain tumor cell lines by (VIIIb), however, at a significantly lower level compared to the natural product (VIIIa). — (MCNULTY, JAMES; MAO, JUSTIN; GIBE, ROMELO; MO, RUOWEI; WOLF, SONJA; PETTIT, GEORGE R.; HERALD, DELBERT L.; BOYD, MICHAEL R.; Bioorg. Med. Chem. Lett. 11 (2001) 2, 169-172; Dep. Chem., Brock Univ., St. Catharines, Ont. L2S 3A1, Can.; EN) 1

ChemInform Abstract: Studies Directed Towards the Refinement of the Pancratistatin Cytotoxic Pharmacophore

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2001 alkaloids

alkaloidsU 0600

17 - 210Studies Directed Towards the Refinement of the PancratistatinCytotoxic Pharmacophore. — The preparation of the deoxy-analogue(VIIIb) of the anticancer/antiviral agent pancratistatin (VIIIa) containing func-tionality complementary to the minimum structural pharmacophore utilizing aDiels–Alder approach is described. Initial anticancer screening of the two deoxy-analogues (VIIIb) and (VIIIc) shows marginal activity for (VIIIc) and selectiveinhibition of certain tumor cell lines by (VIIIb), however, at a significantlylower level compared to the natural product (VIIIa). — (MCNULTY, JAMES;MAO, JUSTIN; GIBE, ROMELO; MO, RUOWEI; WOLF, SONJA; PETTIT,GEORGE R.; HERALD, DELBERT L.; BOYD, MICHAEL R.; Bioorg. Med.Chem. Lett. 11 (2001) 2, 169-172; Dep. Chem., Brock Univ., St. Catharines,Ont. L2S 3A1, Can.; EN)

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