180628-74-4Relevant academic research and scientific papers
Linker Hydrophilicity Modulates the Anticancer Activity of RGD–Cryptophycin Conjugates
Anselmi, Michele,Borbély, Adina,Figueras, Eduard,Michalek, Carmela,Kemker, Isabell,Gentilucci, Luca,Sewald, Norbert
supporting information, p. 1015 - 1022 (2020/12/11)
Most anticancer agents are hydrophobic and can easily penetrate the tumor cell membrane by passive diffusion. This may impede the development of highly effective and tumor-selective treatment options. A hydrophilic β-glucuronidase-cleavable linker was used to connect the highly potent antimitotic agent cryptophycin-55 glycinate with the αvβ3 integrin ligand c(RGDfK). Incorporation of the self-immolative linker containing glucuronic acid results in lower cytotoxicity than that of the free payload, suggesting that hydrophilic sugar linkers can preclude passive cellular uptake. In vitro drug-release studies and cytotoxicity assays demonstrated the potential of this small molecule–drug conjugate, providing guidance for the development of therapeutics containing hydrophobic anticancer drugs.
Synthesis of an Advanced Fragment of (+)-Trienomycinol
Choppin, Sabine,Barbarotto, Marie,Obringer, Michel,Colobert, Fran?oise
, p. 3263 - 3271 (2016/09/09)
The synthesis of the fully functionalized eastern fragment of trienomycins A-F, ansamycin antibiotics is described. A key step involves a peptidic coupling between a sulfonyl aniline and an enantiopure carboxylic acid obtained by a completely diastereosel
Stereochemical assignment of intermediates in the rifamycin biosynthetic pathway by precursor-directed biosynthesis
Hartung, Ingo V.,Rude, Mathew A.,Schnarr, Nathan A.,Hunziker, Daniel,Khosla, Chaitan
, p. 11202 - 11203 (2007/10/03)
Natural and semisynthetic rifamycins are clinically important inhibitors of bacterial DNA-dependent RNA polymerase. Although the polyketide-nonribosomal peptide origin of the naphthalene core of rifamycin B is well established, the absolute and relative c
Total syntheses of (+)-trienomycins A and F via a unified strategy
Smith III,Barbosa,Wong,Wood
, p. 8316 - 8328 (2007/10/03)
The first total syntheses of (+)-trienomycins A and F, representative members of a new class of cytotoxic ansamycin antibiotics, have been achieved. Key features of the unified synthetic scheme included incorporation of the (E,E,E)-triene unit with concom
