Total synthesis of novel dictyostatin analogs and hybrids as microtubule-stabilizing anticancer agents
2009 ◽
Vol 81
(2)
◽
pp. 169-180
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Keyword(s):
Structural modification of the dictyostatin macrolide template through adaptation of our total synthesis has led to the identification of a number of potent analogs of this novel microtubule-stabilizing agent. A common synthetic strategy was exploited, employing a (Z)-selective Still-Gennari olefination between various advanced C11-C26 aldehyde and C4-C10 (or C1-C10) β-ketophosphonate intermediates. In vitro evaluation of the growth inhibitory activity of these analogs against both Taxol-sensitive and -resistant human cancer cell lines has provided a foundation for structure-activity relationship (SAR) studies to help define the pharmacophore region.
2021 ◽
Vol 22
(22)
◽
pp. 12272
2018 ◽
Vol 29
(1)
◽
pp. 131-135
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2008 ◽
Vol 18
(24)
◽
pp. 6451-6453
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Keyword(s):