Human cancer cell lines

YANAGIHARA K, ITO A, TOGE T, NUMOTO M (1993) Antiprolferative effects of isoflavones on human cancer cell lines established from gastrointestinal tract. Cancer Res. 53 5815-21. 

FIGURE 5.35 Growth inhibition assay of three human cancerous cell lines, with dendritic prodrug 38 in the presence ( ) and absence ( ) of PGA cells were incubated for 72 h. 

Table 7.3 shows the concentrations of 1-5 that result in 50% growth inhibition (GI50) of five human cancer cell lines. Inspection of these data reveals that cytostatic activity of 1 and 3-5 depends on the thermodynamic favorability of the quinone methide species compared to the corresponding keto form. The most cytostatic prekinamycins 1 and 5 are associated with the thermodynamically stable quinone methides. In contrast, the inactive prekinamycins 3 and 4 are associated with thermodynamically stable keto tautomers. The exception is prekinamycin 2, which is cytostatic and possesses a relatively stable keto tautomer 3 compared to its quinone methide. Although the AE value for quinone methide tautomerization can predict cytostatic properties, prekinamycin 2 shows that there must be other factors determining biological activity. 

Guerrero, I. C. Andres, L. S. Leon, L. G. Machin, R. P. Padron, J. M. Luis, J. G. Delgadillo, J. Abietane diterpenoids from Salvia pachyphylla and S. clevelandii with cytotoxic activity against human cancer cell lines. J. Nat. Prod. 2006, 69, 1803-1805. 

Human cancer cell lines Ammonium formate On-column LCQ DECA SEQUEST Vollmer et al., 2003) (Xiang et al., 2004)... 

Kawakami, M., Kagotani, K., Okumura, K., Akiyama, S., Kuwano, M., A human canalicular multispecific organic anion transporter (cMOAT) gene is overexpressed in cisplatin-resistant human cancer cell lines with decreased drug accumulation, Cancer Res. 1996, 56, 4124-4129. 

In one recent example of gene expression for pharmacological analysis, Scherf et al. [102] treated 60 different human cancer cell lines with 60,000 compounds. These same 60 cell lines were analyzed by expression analysis [103], and the cell lines were clustered based on expression profiles. The clusters were significantly different from those based on their response to drugs. 

Ross DT et al. Systematic variation in gene expression patterns in human cancer cell lines. Nature Genet 2000 24 227-235. 

Johnston PG, Drake JC, Trepel J et al. Immunological quantitation of thymidylate synthase using the monoclonal antibody TS 106 in 5-fluorouracil-sensitive and -resistant human cancer cell lines. Cancer Res 1992 52 4306-4312. 

This protocol could be extended to a range of different ,/i-unsaturated carbonyl compounds and either activated or deactivated aryl iodides [22], An application of related Heck chemistry to the synthesis of methylated resveratrol (3,4, 5-trihydroxy-( )-stilbene) is shown in Scheme 6.4 [23]. The phytoalexin resveratrol exhibits a variety of interesting biological and therapeutic properties, among them activity against several human cancer cell lines. Botella and Najera have shown that the trimethyl ether of resveratrol (Scheme 6.4) can be rapidly prepared by microwave-assisted Heck reaction of the appropriate aryl iodide and styrene derivatives, using the same oxime-derived palladacycle as indicated in Scheme 6.3. 

Some pyrrolo[2,l-r ][l,2,4]triazines were evaluated against a panel of human cancer cell lines and some of them demonstrated inhibitory effects in the growth of a wide range of cancer cell lines generally at 10 s M concentration and in some cases at micromolar concentrations <2002EJM267, 2002FA97>. 

Mueller H. Kassack M. Wiese M. Comparison of the usefulness of MTT, ATP and calcein assays to predict the potency of cytotoxic agents in various human cancer cell lines. Journal of Biomolecular Screening, 2004, 9,506-515. 

K. Archipelago regulates Cydin F levels in Drosophila and is mutated in human cancer cell lines. Nature 2001,... 

The dimeric carbazole alkaloids often occur along with the corresponding monomeric carbazoles in terrestrial plants [7,62] (Scheme 7). Clausenamine-A was obtained by Wu from the stem bark of Clausena excavata [63]. Clausen-amine-A and its synthetic analogs, like bis(O-demethylmurrayafoline-A), show cytotoxic activities against diverse human cancer cell lines [64] and exhibit moderate antimalarial activity [65,66]. Furukawa isolated l,r-bis(2-hy-droxy-3-methylcarbazole) and bismurrayaquinone-A, the first dimeric car-bazolequinone alkaloid found in nature, from Murraya koenigii [67]. 

After 5 years in the FDA s fast track development program, Romidepsin (Fig. 18) was approved by the FDA for refractory cutaneous T-cell lymphoma on November 6,2009. In the literature, romidepsin has also been called depsipeptide, FK228, FR901228, and NSC-630176. It was isolated from bacterial fermentation extracts from Chromobacterium violaceum and is a potent inhibitor of HDAC. In some human cancer cell lines, romidepsin inhibits HDACs at levels ten times that of TSA. 

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