Leukemia cells cytotoxic activity against

The pyrrolonaphthyridines 208 and 209 can be prepared from rearrangement of the pentacycle 207 upon treatment with trifluoroacetic acid (TFA) (Scheme 52). These products are of interest as they have the same structural skeleton as the indole alkaloid (—)-goniomitine, isolated from the root bark of Gonioma Malagasy <1995JOC3282>. Compound 208 has since been used in the synthesis of further derivatives which show cytotoxic activity against leukemia cells <2001BML79>. 

Imbricatine. C24H26N4O7S, Mr 514.55, a benzyl(tet-rahydro)isoquinoline and imidazole alkaloid from the starfish Dermasterias imbricata. I. is as yet the only alkaloid of this class that does not originate from a plant source. I. induces an escape reaction in the sea anemone Stomphia coccinea when it comes into contact with the starfish. I. has cytotoxic activity against leukemia cell lines. 

Documented effects Compounds isolated from the roots exhibited leishmanicidal activity in vitro and inhibited growth of cultured malaria parasites, human lymphocytes, and human carcinoma cell lines (Sairafianpour et al. 2001). Compounds isolated from the aboveground parts exhibited cytotoxic activity against leukemia cells (Aoyagi et al. 2006). 

Arya and Dandia [26] presented the HY zeolite promoted, environmentally benign solvent free synthesis of 2,4,6-trisubstituted-l,3,5-triazines (xiv) under microwave irradiation. The synthesized derivatives also showed promising activities when screened for phototoxicity and cytotoxic activities against leukemia and adenocarcinoma derived cell lines in comparison to the normal human keratinocytes. 

Camptothecin - An alkaloid from the tree CamPtotheca acuminata, camptothecln ( ) exhibits antineoplastic activity against the mouse leukemias, the plasma cell tumor YPC-1, Walker 256 rat carcinosarcoma and has cytotoxic activity against several cell lines.125-127 Total synthe-sisl28,129 and preliminary structure-activity relationship studiesl30 are reported. Camptothecin is not cross-resistant to leukemias made refractory to the antlfols, 6CNU, cytosine arabinoslde,... 

Haliclonacyclamine F (25), arenosclerin D (26), and arenosclerin E (27) have been recently isolated from the sponge Pachychalina alcaloidifera endemic in Brazil [26]. The alkaloids 25-27 were isolated from the cytotoxic, antibiotic, and antituberculosis MeOH crude extract of P. alcaloidifera by a series of separations on silica-gel and cyanopropyl-bonded silica-gel columns. The structures of compounds 25-27 were established by the same approach employed for the structural elucidation of haliclonacyclamine E (13) and arenosclerins A-C (14-16) [18], as well as by comparison with NMR data for this last series of alkaloids. The alkaloids 25-27 displayed moderate cytotoxic activity against SF295 (human CNS), MDA-MB435 (human breast), HCT8 (colon), and HL60 (leukemia) cancer cell lines. 

A new bromopyrrole alkaloid 15 along with racemic 16 was isolated from the Japanese marine sponge Homaxinellct sp. They exhibit weak cytotoxic activity against P-388 lymphocytic leukemia cells with ED50 values of 21.5 pg/ml and 30 pg/ml, respectively [34]. 

Further examination of cytostatic depsipeptide constituents of the Indian Ocean shell-less mollusc D. auricularia resulted in the isolation of dolastatins 11 (364) (294), 13 (365) together with its dehydro derivative (366) (295), 14 (367) (2%), and 15 (368) (297). Each dolastatin exhibits strong cytotoxic activity against the P388 lymphocytic leukemia cell line, whereas dehydrodolastatin 13 (366) proved to be marginally active. 

Further, eleven 4-phenyl-3,5-diacetyl-1,4-DHPs substituted at the C-4 phenyl ring were synthesized and compared for their cytotoxic activity and MDR reversing activity in in vitro assay systems. Among them, compound G7 (68) showed the highest cytotoxic activity against human promyelocytic leukemia HL-60 and human squamous cell carcinoma HSC-2 cells. However, no compounds tested produced radicals at pH 7.4-12.5. The activity of Pgp... 

Daphneticin (12), isolated from Daphne tangutica, showed cytotoxic activity against Walker carcinosarcoma ascites cells (68) but was inactive against KB cells (68). In vitro studies showed cleomiscosin A (9), isolated from the chloroform extract of Brucea javanica, to be active against the murine P-388 lymphocytic leukemia cell line (EDsq = 0.4 pg ml ), but inactive against the KB test system (57). Luyengi et al. reported the lack of activity of the same compound when evaluated against HL-60 human promyelocytic leukemia cells (59). 

It possessed cytotoxicity for six cell lines (IC50 l 100pg/mL) and antitumor effects on human nasopharyngeal cancer (CNE2, SUNE-1) and human liver cancer (BEL-7402) in nude mice. Recently artesunate has been analyzed for its antitumor activity against 55 cell lines.It was most active against leukemia and colon cancer cell lines. It is notable that no CEM leukemia sublines, which are resistant to either doxorubicin, vincristine, methotrexate, or hydroxyurea, showed cross resistance to artesunate. 

Two new lavandulylated flavanones (2S)-2/-methoxykurarinone (67) and (-)-kurarinone (68)—found in the root of Sophora flavescens—were determined together with two lavandulyl flavanones sophoraflavanone G (10) and leachi-anone A (66), and two isoflavonoids formononetin (4) and 1-maackiain (6). Four flavanones (3, 66, 67, and 68) exhibited significant cytotoxic activity against human myeloid leukemia HL-60 cells (Fig. 14) [12,13]. 

Berberine chloride was demonstrated to possess significant cytotoxic activity against cultured P-388 (murine lymphocytic leukemia) cells, in addition to three human cancer cell lines BC1 (breast cancer) - EDJ0 2.7 pM) HT-1080 (fibrosarcoma) - ED50 2.4 pM) and KB (nasopharyngeal carcinoma) - EDJ0 8.4 pM)[336]. 

Berberrubine chloride was found to exhibit cytotoxic activity against cultured P-388 (murine lymphocytic leukemia) cells (1.7 pM)[336]. 

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