One of our aims in pursuing the total synthesis of celogentin C was to prepare sufficient quantities of the natural product to enable anticancer screening. Kobayashi and coworkers demonstrated its potency as an antimitotic agent, 4 but prior to our work, there were no reports of its efficacy in antiproliferative assays employing cancer cells. We were able to synthesize a batch of material that was large enough for screening against the 60-cell-line panel of the National Cancer Institute.
Project I Celogentin C, isolated by Kobayashi from the seeds of Celosia argentea in 2001 exhibits strong inhibitory behavior towards polymerization of tubulin – globular protein, which plays crucial role during the cell division cycle. Mar 16, 2006 · Celogentin C (1, Figure 1) is a bicyclic octapeptide isolated by Kobayashi from the seeds of Celosia argentea.1It is a member of a growing family of structurally similar bicyclic peptides including moroidin2and celogentins A–J3as well as the related monocyclic peptides celogentin K4and stephanotic acid.5Many of these natural products inhibit the polymerization of tubulin,6with 1ranking as the most potent agent of this class of compounds. Dec 17, 2019 · Abstract Bicyclic analogues of celogentin C have been synthesized in which the side chain–side chain cross‐links are replaced by thioether bonds. Several of the simplified bicyclic peptides displayed potent inhibition of tubulin polymerization. Project ICelogentin C, isolated by Kobayashi from the seeds of Celosia argenteain 2001 exhibits strong inhibitory behavior towards polymerization of tubulin – globular protein, which plays crucial role during the cell division cycle. We have attempted synthesis of the left- In the course of a synthesis of the bicyclic nonribosomal peptide Celogentin C, isolated from the seeds of the plumed cockscomb Celosia argentea, Gong Chen of Pennsylvania State University took advantage (Angew. Chem.
Jan 19, 2010 · Abstract A total gent : Inspired by the biosynthesis of celogentin C, a highly stereoselective and efficient palladium‐catalyzed C H functionalization strategy is employed to construct the key Leu‐Trp linkage of this bicyclic compound. A streamlined synthesis is completed in 23 steps from simple amino acid building blocks.
2018-2-1 · C—H键是有机化合物中存在最广泛的化学键之一, 从最简单的甲烷到复杂的药物分子、生物大分子都含有大量的C—H键. C—H活化是通过断裂未活化的C—H键, 然后再在某个特殊的位点形成新的C—C键或者C—杂原子键(狭义上未活化C—H键是指pK a ＞25的C—H键).这种方法可以避免传统合成中的 … 贾彦兴_百度百科 2019-8-2 · Acid Methyl Ester and (–)-Celogentin C”, Weimin Hu, Fengying Zhang, Zhengren Xu, Qiang Liu, Yuxin Cui, Yanxing Jia*. Org. Lett. 2010, 12, 956-959. 2. “Water-Controlled Regioselectivity of Pd-Catalyzed Domino Reaction Involving a C–H 973标书 2010CB833200-具有重要生物活性的天然 …
2014-10-21 · Our synthetic plan of celogentin C is outlined in Scheme 1.A left-to-right sequence was adopted. The Trp-His C–N coupling and the final construction of the right-hand ring of 4 would follow the elegant sequence reported by Castle. The formation of the left-hand ring would be considered as the total synthesis of stephanotic acid methyl ester 12, which could be achieved by macrolactamization
Antimicrobial activity of simpliﬁed mimics of celogentin C Varsha J. Thombare a, b, James A. Holden b, c, Sreetama Pal d, e, Eric C. Reynolds b, c, Amitabha Chattopadhyay e, f, Neil M. O'Brien-Simpson b, c, Craig A. Hutton a, b, * a School of Chemistry, The University of Melbourne, Victoria 3010, Australia