On June 21, 2003, Kuehne, Martin E.; Bornmann, William G.; Marko, Istvan; Qin, Yong; LeBoulluec, Karen L.; Frasier, Deborah A.; Xu, Feng; Mulamba, Tshilundu; Ensinger, Carol L.; Borman, Linda S.; Huot, Anne E.; Exon, Christopher; Bizzarro, Fred T.; Cheung, Julia B.; Bane, Susan L. published an article.Related Products of 42900-89-0 The title of the article was Syntheses and biological evaluation of vinblastine congeners. And the article contained the following:
Sixty-two congeners of vinblastine (VLB), e.g. I, , primarily with modifications of the piperidine ring in the carbomethoxycleavamine moiety of the binary alkaloid, were synthesized. For example, I was prepared starting from δ-valerolactone (II). Methylation of II at the 3-position followed by ring opening gave MeO2CCH(Me)CH2CH2CHO which was reacted with indoloazepine III. The resulting bridged indoloazepine was N-benzylated to give pyrrolocarbazolecarboxylate IV. IV then went through a series of reactions, including addition to vindoline to give I in 81% yield. These compounds were evaluated for cytotoxicity against murine L1210 leukemia and RCC-2 rat colon cancer cells, and for their ability to inhibit polymerization of microtubular protein at <10-6 M, and for induction of spiralization of microtubular protein, and for microtubular disassembly at 10-4 M concentrations An ID50 range of >107 M concentrations was found for L1210 inhibition by these compounds, with the most active 1000× as potent as vinblastine. The experimental process involved the reaction of Isochroman-3-ol(cas: 42900-89-0).Related Products of 42900-89-0
The Article related to vinblastine congener preparation antitumor, microtubular disassembly spiralization induction polymerization inhibition vinblastine congener, spiralization induction microtubular vinblastine congener, polymerization inhibition microtubular vinblastine congener, colon adenocarcinoma inhibition vinblastine congener and other aspects.Related Products of 42900-89-0
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