Cell growth inhibitors

Tuckmantel, W., Kozikowski, A.P., and Romanczyk, L.J. Jr., Studies in polyphenol chemistry and bioactivity. 1. Preparation of building blocks from (+)-catechin. Procyanidin formation. Synthesis of the cancer cell growth inhibitor, 3-0-galloyl-(2R,3R)-epicatechin-4(3,8-[3,0-galloyl-(2R,3R)-epicatechin], J. Am. Chem. Soc., 121, 12073, 1999. 

There are many natural and biological macromolecules that possess anticancer activity. Cytokines, topoisomerase inhibitors, monoclonal antibodies, thymic hormones, cell growth inhibitors, and enzymes have been used [68], They have been recently reviewed [59,69] and their detailed description is beyond the scope of this article. The main problems connected with the administration of such natural macromolecules is their short intravascular half-life, immunogenicity, and sometimes poor solubility. Their modification with synthetic macromolecules can dramatically increase their therapeutic potential as described below. 

Pettit, G. R., Herald, C. L., Cichacz, Z. A., Gao, F., Schmidt, J. M., Boyd, M. R., Christie, N. D., and Boettner, F. E., Isolation and structure of the powerful human cancer cell growth inhibitors spongist-atins 4 and 5 from an African Spirastrella spinispirulifera (Porifera), J. Chem. Soc., Chem. Commun., 1805, 1993. 

Using this strategy, it is possible to find leads that are both active cell growth inhibitors and are also specific to a molecular target known beforehand (DeVito et al., 2002). DeVito and coworkers screened the reference strains (parent strains used for genetic manipulations) and the underexpression strains (such as ImurA and ImetG) against the same compound library. Hit compounds... 

G.R. Pettit and co-workers converted a highly substituted frans-stilbene derivative to the strong cancer cell growth inhibitor and antimitotic agent hydroxyphenstatin. The key step of the synthesis was a BFs-OEta-catalyzed pinacol rearrangement of an optically active vicinal diol to afford a substituted diphenylacetaldehyde in racemic form. From this key intermediate, several derivatives were prepared in addition to the target molecule. 

Carbazilquinone was very effective against the intramuscular (i.m.) Ehrlich ascites tumor when used with local hyperthermia (37-41°) and temporary interruption of blood flow.15 Mature ribosome formation was blocked by BCNU indicating that the effectiveness of this drug as a cell growth inhibitor may be due to the inhibition of protein synthesis. 6 A new nitrosourea glucoside had activity which was comparable to that of... 

P-Keto acid 128 and dipeptide 129 are successfully coupled in the presence of DEPC to afford dolastatin 18 (130, Dhex-(S)-Leu-Af-Me-(/ )-Phe-Doe) in 60% yield.S2 The structure of cell growth inhibitor dolastatin 18 is confirmed by X-ray crystal studies. 

The most significant group of bioactive metabolites to be isolated from southern African marine worms have undoubtedly been the powerful cell growth inhibitors, cephalostatins 1-17 (1-17), isolated by Pettit et al. from... 

A phase-transfer catalyzed a-alkylation of 374 was also one of the key steps in the first total synthesis of (—)-antofine (398) by Kim et al. 347). The naturally occurring phenanthroindolizidine alkaloid (—)-antofine (398) is a highly potent cancer cell growth inhibitor with ICso values in the low nanomolar range 348). The stereogenic center could be installed by reacting 374 with electrophile 399 in the presence of the dimeric catalyst 391 (Scheme 89). With the key intermediate 400 in hand, final manipulations to obtain the natural product 398 were then achieved in a straightforward manner (547). 

Pettit GR, Cichacz ZA, Gao F, Herald CL, Boyd MR (1993) Isolatirm and Structure of the Remarkable Human Cancer Cell-Growth Inhibitors Sptmgistatin-2 and Sptmgistatin-3 from an Eastern Indian Ocean-Spongia sp. J Chem Soc, Chem Corrrmun 1166... 

Tri-0-acetyl-j8-D-ribofuranosyl)-l,2,3-triazole-4,5-dicarbonitrile 1386, an analogue of the human myeloid leukemia cell growth inhibitor Ribavirin 1384, has been prepared from its carboxamide 1385 by dehydration with phosgene [1050). 

Tumbas Saponjac, V., Canadanovic-Brunet, J., Ceflcovic, G., Djilas, S., Cetojevic-Simin, D. (2015) Dried bilberry (Vaccinium myrtillus L.) extract fractions as antioxidants and cancer cell growth inhibitors. LWT - Food Science and Technology. ISSN 00236438. DOI 10.1016/j.lwt.2014.04.021... 

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