Anti-proliferative activity

Pihie AHL, Stanslas J, Din LB. Non-steroid receptor-mediated anti-proliferative activity of styrylpyrone derivative in human breast cancer cell lines. Anticancer Res 1998 18 1739-1743. 

Roy MK, Takenaka M, Isobe S and Tsushida T. 2007. Antioxidant potential, anti-proliferative activities, and phenolic content in water-soluble fractions of some commonly consumed vegetables effects of thermal treatment. Food Chem 103(1) 106-114. 

Most cytokines are pleiotropic, i.e. can affect a variety of cell types. Moreover, the effect that a cytokine has on one cell type may be the same or different to its effect on a different cell type. IL-1, for example, can induce fever, hypotension and an acute phase response. G-CSF is a growth factor for neutrophils, but it is also involved in stimulating migration of endothelial cells and growth of haematopoietic cells. IFN-y stimulates activation and growth of T- and B-lymphocytes, macrophages, NK cells, fibroblasts and endothelial cells. It also displays weak anti-proliferative activity with some cell types. 

IFN-y exhibits, at best, weak antiviral and anti-proliferative activity. When co-administered with type I interferons, however, it potentates these IFN-a/p activities. IFN-y is directly involved in regulating most aspects of the immune and inflammatory responses. It promotes activation, growth and differentiation of a wide variety of cell types involved in these physiological processes (Table 8.7). 

The antiviral and anti-proliferative activity of interferons, as well as their ability to modulate the immune and inflammatory response renders obvious their potential medical applicatioa This has culminated in the approval for clinical use of several interferon preparations (Table 8.8). Ongoing clinical trials are likely to expand the medical uses of these regulatory molecules further over the next few years. 

GlaxoSmithKline has filed patent applications covering 5-(benzimidazol-l-yl)thiophenes 111 and 112 and 2-(benzimidazol-l-yl)thioazoles 113 as inhibitors of PLK-1 [274,275]. Many potent compounds were claimed for 5-(benzimidazol-l-yl)thiophene series, including analog 111 with submicromolar inhibition against PLK-1 and anti-proliferative activity in five out of the six tumor cell lines tested. According to the data disclosed in the filing, a variety of substituents were accommodated on the 5- and 6-positions of the ben-... 

A GlaxoSmithKline patent reported a series of imidazo[5,l-/] [1,2,4]triazines to have activity against PLK-1 [276]. The most potent analogs, exemplified by compounds 114a,b, were active against PLK-1 in the submicromolar range and had anti-proliferative activity with IC50 values of 1 to 10 tiM. The preferred 2-substituents on the imidazotriazine core were the 3,4,5 trimethoxyaniline and M(4-amino-phenyl)acetamide, while the preferred 7-substituents were phenyl and meta-trifluoromethylphenyl. 

Assert R, Kotter R> Bisping G, Scheppach W, Stahlnecker E, Miiller KM, Dusel G, Schatz H, Pfeiffer A (1999) Anti-proliferative activity of protein kinase C in apical compartments of human colonic crypts evidence for a less activated protein kinase C in small adenomas. Int J Cancer 80 47-53 Azuma Y, Onishi Y, Sato Y, Kizaki H (1993) Induction of mouse thymocyte apoptosis by inhibitors of tyrosine kinases is associated with dephosphorjdation of nuclear proteins. Cell Immimol 152 271-278... 

Not all type I IFNs induce exactly the same range of responses, and the anti-viral anti-proliferative activity ratio differs from one type IIFN to another. As all bind the same receptor, the molecular basis by which variation in biological activities is achieved, is poorly understood as yet. 

More recently fluoromethylene deoxycytidines have been rationally designed by McCarthy et al. as bio-precursors of mechanism-based inhibitors of RDPR, after phosphorylation in vivo by the deoxycytidine kinase. Among these, tezacita-bine (MDL 101731) [92] has a high anti-proliferative activity and is currently in clinical phase III evaluation for the treatment of solid tumours [92],... 

From this success, further efforts have been focused on dissociating the calcemic activity from the anti-proliferative activity, with the aim to limit the former... 

A set of N1-unsubstituted furo[2,3- ]quinolin-2(l/f)-ones including 81a-c, 83, and 84a and 84b were prepared by the route shown in Scheme 11, and their photobiological activities were compared with those of the photoche-motherapeutic drugs 4,6,8,9-tetramethylfuro[2,3-, ]quinolin-2(l//)-one (HFQ) and 8-methoxypsoralen 8-MOP <2002BMC2835>. The anti-proliferative activity of these furoquinolinones was tested upon UVA irradiation in mammalian cells, and almost all were found more active than 8-MOP, and free of any mutagenic activity and skin phototoxicity. 

Maloney, D. G., Smith, B., and Appelbaum, F. R. (1996). The anti-tumor effect of monoclonal anti-CD20 antibody therapy includes direct anti-proliferative activity and induction of apoptosis in CD20 positive non-Hodkin s lymphoma cell lines. Blood 88, 637a. 

Dasgupta P, Singh A, Mukherjee R (2002) N-terminal acylation of somatostatin analog with long chain fatty acids enhances its stability and anti-proliferative activity in human breast adenocarcinoma cells. Biol Pharm Bull 25 29-36 Delgado C, Francis GE, D. F (1992) The uses and properties of PEG-linked proteins. Crit Rev Ther Drug Carrier Syst 9 249-304... 

Lemke J, Pinto A, Niehoff P, Vasylyeva V, Metzler-Nolte N (2009) Synthesis, structural characterisation and anti-proliferative activity of NHC gold amino acid and peptide conjugates. Dalton Trans 7063-7070... 

NPs was measured by E2 binding competition in MELN cells. Notwithstanding potential dmg adsorption at the NP surface, 5 and 35 were incorporated efficiently in NC and NS, which slowly released both compounds. When incubated with MCF-7 cells, they arrested the cell cycle in the S-phase and induced apoptosis, and these effects were enhanced when the compounds were encapsulated in NS. A decrease in their anti-proliferative activity in the presence of the anti-oxidant-tocopherol indicated that the production of ROS may be involved in the cytotoxic mechanism. 

---