2426-84-8Relevant articles and documents
Mussel-inspired healing of a strong and stiff polymer
Chen, Ning,Qin, Liming,Pan, Qinmin
, p. 6667 - 6674 (2018)
Self-healability will greatly improve the reliability, service life and maintenance of synthetic materials. However, it remains a big challenge to realize the self-healing of a strong and stiff polymer due to its poor molecular mobility. Inspired by the h
Synthesis and in-vitro anti-hepatitis-B virus activity of 6H-[1]benzothiopyrano[4,3-b] quinolin-10-ols
Jia, Wei,Zhao, Yanfang,Li, Rongdong,Wu, Yanjiao,Li, Zebiao,Gong, Ping
, p. 507 - 512 (2009)
A series of 9-methoxy-6H-[1]benzothiopyrano[4,3-b]quinolin-10-ols with a Mannich side chain were synthesized and evaluated for their anti-Hepatitis B virus (HBV) activity in HepG2.2.15 cells. Some compounds showed significant anti-HBV activity with IC50 values less than 41 μM. Among them, compound 9b was the most effective anti-HBV agent (IC50 = 1.7 μM, SI = 60.3).
Synthesis and biological evaluation of a novel C8-pyrrolobenzodiazepine (PBD) adenosine conjugate. A study on the role of the PBD ring in the biological activity of PBD-conjugates
Bhakta, Sanjib,Brucoli, Federico,Ferguson, Lindsay,Fox, Keith R.,Wells, Geoff
, (2020/03/19)
Here we sought to evaluate the contribution of the PBD unit to the biological activity of PBD-conjugates and, to this end, an adenosine nucleoside was attached to the PBD A-ring C8 position. A convergent approach was successfully adopted for the synthesis of a novel C8-linked pyrrolo(2,1-c)(1,4)benzodiazepine(PBD)-adenosine(ADN) hybrid. The PBD and adenosine (ADN) moieties were synthesized separately and then linked through a pentynyl linker. To our knowledge, this is the first report of a PBD connected to a nucleoside. Surprisingly, the compound showed no cytotoxicity against murine cells and was inactive against Mycobacterium aurum and M. bovis strains and did not bind to guanine-containing DNA sequences, as shown by DNase I footprinting experiments. Molecular dynamics simulations revealed that the PBD-ADN conjugate was poorly accommodated in the DNA minor groove of two DNA sequences containing the AGA-PBD binding motif, with the adenosine moiety of the ligand preventing the covalent binding of the PBD unit to the guanine amino group of the DNA duplex. These interesting findings shed further light on the ability of the substituents attached at the C8 position of PBDs to affect and modulate the biological and biophysical properties of PBD hybrids.
POLYCYCLIC AMIDES AS CYTOTOXIC AGENTS
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Page/Page column 175, (2020/03/29)
The invention relates to a compound of formula (I): or pharmaceutically acceptable salts, solvates, tautomers, stereoisomers or mixtures thereof; wherein the fused ring moiety is a non-alkylating moiety; and wherein the compounds are useful as medicaments, in particular for use as a drug in an antibody-drug conjugate and in the treatment of a proliferative disease, a bacterial infection, a malarial infection and inflammation.