NCI 60 cells

O Neill and coworkers have also sought to address the problem of the metabolically susceptible CIO acetal linkage . A series of CIO carba dimers were prepared and assayed for antitumour activity. The two most potent compounds that were prepared are two phosphate ester finked dimers 115 and 116 (Scheme 40). They are principally active against leukaemia, colon and certain melanoma and breast cancer cell lines in the NCI 60-cell line assay. 

The cyclic hexapeptide, waiakeamide (447) was isolated from an Indonesian collection of Ircinia dendroides [373]. Haliclona nigra from Papua New Guinea contained two cyclic hexapeptides, haligramides A (448) and B (449). They showed an unusual activity pattern in the National Cancer Institute (NCI) 60 cell-line panel [374],... 

In another example, real-time polymerase chain reaction (RT-PCR) was used to determine expression levels of the 48 known human ABC-type transporters in the NCI-60 cell lines, and these levels were correlated with sensitivity to 1429 candidate anticancer drugs (149, 150). Patterns of expression correlated moderately well with tissue of origin and were independent of sequence homology among... 

Two new cyclic heptapeptides, scytalidamides A 43 and B 44, were isolated from the culture broth of a marine fungus, Scytalidium sp., collected from the Bahamas. Compounds 43 and 44 showed moderate in vitro cytotoxicity toward HCT-116 human colon adenocarcinoma with IC50 values of 2.7 and 11.0 pM, respectively. Both compounds displayed moderate cytotoxicity in the NCI 60 cell-line panel with mean GI50 values of 7.9 and 4.1 pM for 43 and 44, respectively. The most sensitive cell lines were MOLT-4 leukemia (3.0 pM) for 43 and Uacc-257 melanoma (1.2 pM) for 44. The total syntheses of scytalidamide A 43 was achieved on solid phase using two different resins, a phenylalanine silane resin and a 4-methoxybenzaldehyde backbone linker resin. ... 

Cephalostatin 1 (repeatedly the most active in the series) has recently been shown to induce a novel pathway of receptor-independent apoptosis of leukaemia cells at nanomolar concentrations [26]. Given the unique profile of activity of 1 in the NCI 60 cell line screen, this compound was identified in 2000 as a Rapid Access to Intervention Development (RAID) project by the NCI [27], Unfortunately, preclinical development... 

Compound Yield GI NCI 60 cell line screen ICso inhibition of tubulin polymerization... 

The N,N-dimethyl derivatives (17, 18) were tested against the American National Cancer Institute (NCI) 60 cell line panel but no useful selectivity was found [28]. 

Although the CHCls-soluble extracts were not found to be significantly cytotoxic (ED50 >20 M,g/ml), the lupane-type triterpenoid lactones were tested in a panel of human cancer cell lines. In this case it was reported, that compounds 128 and 135 were modestly cytotoxic, while 129 and 136 were not active in the panel (Table 5). On being evaluated in the National Cancer Institute (NCI) 60-cell line human tumor panel, as well as in a newly developed hollow fiber assay, ochraceolide A has been selected for in vivo evaluation at the NCI in several murine xenograft systems. 

Cephalostatin 1 (119) is among the most powerful anticancer agents ever tested, displaying subnanomolar-to-picomolar cytotoxicity against much of the National Cancer Institute s (NCI) 60-cell line panel, with femtomolar activity against the P388 cell line and in the Purdue Cell Culture Laboratory (PCCL) human tumor panel [109,110]. 

Surprisingly, the analog 4.2.2.12 was almost half as cytotoxic as taxol in two different cell lines and in a tubulin-assembly assay, and it also showed a similar pattern of cytotoxicity to taxol in the NCI 60-cell line panel. These findings indicate that an intact C-ring is not an absolute requirement for activity. This result has been discussed by Snyder, who has provided a model to explain why only compounds with 3 -alkyl chains are active in this series 184). 

Antiproliferative activities of these structures have been evaluated in vitro against the NCI 60-cell line panel of human malignant cells [125]. The best total growth inhibition (TGI) activities on the 60-cell line were obtained for the phosphinate series 142, 143 with values of 38.1 pM for 142a and 29.2 pM for 143c. Tetrahydrophosphinines 144-Et, 144-Bn and 145 were less active. In parallel. 

Ko, D. Xu, W. Windle, B. (2005). Gene Function Classification Using NCI-60 Cell Line Gene Expression Profiles. Computational Biology and Chemistry, Vol. 29, p>p. 412-419. 

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