- In pursuit of balgacyclamide A – Discovery of an oxazoline macrocycle with multiple myeloma cytotoxicity and penetration
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Four new oxazoline based macrocycles have been constructed, said cycles were found to possess varying cytotoxicity against six different cancer cell lines: IC50 values of 6.4 μM towards HeLa and 11.9 μM towards LnCaP being the most potent. Two of the four macrocycles were found to have marginal cytotoxicity against MM.1S and MM.1R, myeloma cancer cell lines, and further evaluation showed that they also possessed rapid cellular uptake and accumulation characteristics. Through the structure-activity relationship comparisons between the four compounds, it was found that the C6 position of the E-ring is amendable to substitution and could possibly serve as a conjugation site for the development of a selective delivery system to MM.1R.
- Hoang, Vinh L.,Zhang, Yichao,Rafferty, Ryan J.
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- Total synthesis of wewakazole B
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Wewakazole B is a novel cyclodecapeptide with highly potent cytotoxic activity isolated from a sample of M. producens collected from the Red Sea. It contains nine common and three modified amino acid residues. The first total synthesis of Wewakazole B was successfully achieved on a gram scale, unambiguously confirming its structure. Notable features include the careful choice of amino acid-protecting groups and the construction of three different substituted oxazoles present in this natural product.
- Long, Bohua,Zhang, Jingzhao,Tang, Xudong,Wu, Zhengzhi
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supporting information
p. 9712 - 9715
(2016/10/31)
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- PYRAZOLOPYRIMIDINE COMPOUNDS AND THEIR USE AS PDE10 INHIBITORS
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The present invention relates to a compound represented by formula [I]: wherein: R1 is hydrogen, halogen, lower alkyl or cyano; Ring A is an optionally substituted heterocyclic group; Ring B is an optionally substituted 3 to 6-membered monocyclic group; and Y is optionally substituted amino, optionally substituted cyclic amino, optionally substituted aliphatic 3 to 6-membered monocyclyloxy, optionally substituted lower alkyl or optionally substituted lower alkyl-O-, or a pharmaceutically acceptable salt thereof, and to their use as PDE10 inhibitor.
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Page/Page column 86
(2011/09/30)
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- High yielding synthesis of dehydroamino acid and dehydropeptide derivatives
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By using a 4-dimethylaminopyridine (DMAP) catalysed reaction of β-hydroxyamino acid derivatives with tert-butyl pyrocarbonate [(Boc)2O], dehydroamino acid derivatives are obtained in high yields. The same methodology applied to dipeptides with
- Ferreira, Paula M.T.,Maia, Hernani L.S.,Monteiro, Luis S.,Sacramento, Joana
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p. 3697 - 3703
(2007/10/03)
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