198632-67-6Relevant articles and documents
A Mutasynthesis Approach with a Penicillium chrysogenum ΔroqA Strain Yields New Roquefortine D Analogues
Ouchaou, Kahina,Maire, Florian,Salo, Oleksandr,Ali, Hazrat,Hankemeier, Thomas,Van Der Marel, Gijsbert A.,Filippov, Dmitri V.,Bovenberg, Roel A. L.,Vreeken, Rob J.,Driessen, Arnold J. M.,Overkleeft, Herman S.
, p. 915 - 923 (2015)
Penicillium chrysogenum, which lacks the roqA gene, processes synthetic, exogenously added histidyltryptophanyldiketopiperazine (HTD) to yield a set of roquefortine-based secondary metabolites also produced by the wild-type strain. Feeding a number of synthetic HTD analogues to the ΔroqA strain gives rise to the biosynthesis of a number of new roquefortine D derivatives, depending on the nature of the synthetic HTD added. Besides delivering semisynthetic roquefortine analogues, the mutasynthesis studies presented here also shed light on the substrate preferences and molecular mechanisms employed by the roquefortine C/D biosynthesis gene cluster, knowledge that may be tapped for the future development of more complex semisynthetic roquefortine-based secondary metabolites.
MITHRAMYCIN DERIVATIVES HAVING INCREASED SELECTIVITY AND ANTI-CANCER ACTIVITY
-
Paragraph 0097, (2019/04/05)
Mithramycin side chain carboxylic acid (MTM-SA) derivative are provided, which include a substituted amino acid derivative, a substituted amino acid dipeptide derivative, or an unsubstituted dipeptide derivative. The MTM-SA derivatives are useful for treatment of cancer or neuro-diseases associated with an aberrant erythroblast transformation-specific transcription factor. Unique MTM-SA derivatives have increased selectively toward ETS transcription factor.
Diketo acids and their amino acid/dipeptidic analogues as promising scaffolds for the development of bacterial methionine aminopeptidase inhibitors
Masood, Mir Mohammad,Pillalamarri, Vijay K.,Irfan, Mohammad,Aneja, Babita,Jairajpuri, Mohamad Aman,Zafaryab,Rizvi, M. Moshahid A.,Yadava, Umesh,Addlagatta, Anthony,Abid, Mohammad
, p. 34173 - 34183 (2015/04/27)
Using diketoesters as the template, various derivatives were designed and the selected compounds were synthesized as bacterial methionine aminopeptidase (MetAP) inhibitors. The results of in vitro antibacterial screening revealed fifteen compounds (1a-c,