scholarly journals Synthesis and biological activity of a new type of PM-toxin analogue containing oxygen atoms in the carbon-chain skeleton.

1989 ◽  
Vol 53 (2) ◽  
pp. 453-459 ◽  
Author(s):  
Yoshikatsu SUZUKI ◽  
S. J. DANKO ◽  
Yoshiki KONO ◽  
J. M. DALY ◽  
H. W. KNOCHE ◽  
...  
1989 ◽  
Vol 53 (2) ◽  
pp. 453-459
Author(s):  
Yoshikatsu Suzuki ◽  
S. J. Danko ◽  
Yoshiki Kono ◽  
J. M. Daly ◽  
H. W. Knoche ◽  
...  

2014 ◽  
Vol 82 ◽  
pp. 172-180 ◽  
Author(s):  
En-Jun Gao ◽  
Hong Fu ◽  
Ming-Chang Zhu ◽  
Chi Ma ◽  
Shi-Kai Liang ◽  
...  

1972 ◽  
Vol 32 (4) ◽  
pp. 1146-1146 ◽  
Author(s):  
Shinya Hashimoto ◽  
Hiroshi Iwasaki ◽  
Shiro Ogawa ◽  
Sadae Yamaguchi ◽  
Makoto Hirabayashi

2019 ◽  
Vol 43 (46) ◽  
pp. 18229-18239 ◽  
Author(s):  
Ambrósio Camuenho ◽  
A. Jorge Parola ◽  
Alfonso Alejo-Armijo ◽  
Ramesh Pandian ◽  
Clara S. B. Gomes ◽  
...  

Amino-substituted pyridinechalcones configure multistate systems where a new type of flavylium derivative with potential biological activity are present.


1993 ◽  
Vol 58 (9) ◽  
pp. 2159-2179 ◽  
Author(s):  
Miroslav Otmar ◽  
Ivan Rosenberg ◽  
Milena Masojídková ◽  
Antonín Holý

[5-(Adenin-9-yl)-5-deoxypentofuranosyl]phosphonates, a new type of nucleotide analogs with fixed HPMPA structure, have been prepared. The synthesis of compounds of L-arabino (IIa, IIb), D-arabino(XIVa, XIVb), 2-deoxy-L-erythro(IIIa, IIIb) and 2-deoxy-L-threo(IVa, IVb) configuration is based on the Michelis-Arbuzov reaction of the fully protected methyl glycosides with triethyl phosphite and trimethylsilyl triflate which leads to anomeric mixture of diethyl (L-pentofuranosyl) phosphonates. The protected 5-O-tosyl derivatives react with sodium salt of adenine to give N9-substituted products which after total deprotection afforded the tittle nucleotide analogs. The fixation of the partial structure of HPMPA to form five-membered ring leads to a significant decrease, or a total loss, of biological activity.


1. In a recent paper on the structure of certain silicates, Prof. W. L. Bragg and one of the authors discussed in considerable detail the role which the oxygen atoms—due to their relatively large size—played in these compounds. The structures examined fell roughly into two classes: one in which the O atoms were throughout packed as closely together as possible, the other in which close packing was local only. Many examples of structures which had actually been worked out were given, and it was suggested that topaz might possibly prove a further example of a close-packed arrangement of large ions. An attempt to solve the structure of topaz on these lines proved unexpectedly difficult, and a detailed general quantitative examination was therefore carried out. A full account of this examination, which has now been completed, will be published later in the 'Zeitschrift für Kristallographie.’ We propose here to give but a general outline of the structure, desiring rather to draw attention to an interesting new type or variant of close packing which the study has revealed, and which suggests important considerations in the elucidation of complex structures still awaiting analysis.


Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5775
Author(s):  
Simeng Xu ◽  
Yufang Cao ◽  
Yu Luo ◽  
Di Xiao ◽  
Wei Wang ◽  
...  

Among the known biguanide drugs, proguanil has the best antiproliferative activity. In contrast, newly synthesized biguanide derivatives containing fluorine atoms have excellent biological activity, among which trifluoromethoxy compounds show the strongest ability. Preliminary work in our laboratory exhibited that n-heptyl containing proguanil derivatives on one alkyl chain side have better biological activity than those with a shorter carbon chain. However, the relationship between the length of the carbon chain and the activity of the compounds is unknown. In this study, we synthesized 10 new trifluoromethoxy-containing proguanil derivatives with various carbon chain lengths. The phenyl side is fixed as the trifluoromethoxy group with change of carbon chain length in alkyl chain side. It was found that the anti-cancer abilities of 5C–8C with n-pentyl to n-octyl groups was significantly better than that of proguanil in the five human cancer cell lines. The colony formation assay demonstrated that 6C–8C at 0.5 to 1.0 μM significantly inhibited the colony formation of human cancer cell lines, much stronger than that of proguanil. Pharmacologically, 8C activates AMPK, leading to inactivation of the mTOR/p70S6K/4EBP1 pathway. Thus, these novel compounds have a great potential for developing new anti-cancer candidates.


Sign in / Sign up

Export Citation Format

Share Document