Leukemia cells, inhibitory activity against

In 1991, Kojiri et al. reported the isolation of BE-13793C (344), an alkaloid isomeric with the arcyriaflavins C (347) and D (348) (see Scheme 2.89), from the culture broth of Streptoverticillium moharaense strain BA 13793 collected in Seto, Aichi Perfecture, Japan. BE-13793C (344) showed strong inhibitory activity against topoisomerases I and II and inhibited the growth of doxorubicin-resistant or vincristine-resistant P-388 murine leukemia cell lines, as well as their parent P-388 cell line (330). 

Macrosphelides (macrosphelide A, 115) are 16-membered ring macrotriolides isolated by Microsphaeropsis sp. [144]. Compound 115 showed potent inhibitory activity against cell adhesion of human leukemia cells (HL-60) to LPS-activated... 

Maduropeptin is a complex of new chromoprotein antitumor antibiotics isolated from Ac-tinomadura madurae (ATCC 39144) in 1990 [35, 36], It exhibits potent inhibitory activity against Gram-positive bacteria and tumor cells and strong in-vivo antitumor activity in P388 leukemia and B16 melanoma implanted mice. The structure of the chromophore has been recently elucidated [36], confirming it as a member of the family of enediyne antibiotics, and will be published shortly. 

Dichotomins A, B, C, and E showed cell growth inhibitory activities against p388 lymphocytic leukemia cells (IC50 A 2.5 /xg/ml B 3.5 pg/ml C 5.0 /xg/ml E 2.0 jug/ml) dichotomin D did not. The amino acid sequences of dichotomins A, B, and C are the same, except at residue 5 (dichotomins A Val B Thr C Ala). The cyclic pentapeptide, dichotomin E, contains a sequence (Tyr-Ala-Phe) similar to the Phe-Leu-Tyr sequence present in dichotomins A, B, and C, the central aliphatic amino acid of which is sandwiched between two aromatic amino acids. This inhibitory activity may be due to the sequencing and/or conformation of these dichotomins. 

Bogert and Hand used 2-aminobenzonitrile derivatives to generate 2-styrylquinazoline-4(3//)-one analogues. Treatment of 2-aminobenzonitrile with 3-phenyl-acryloyl chloride followed by oxidative ring closure, gave the desired quinazolinone in 29% yield. 6-Chloro derivatives of this class of compounds, independently prepared by Hamel and co-workers (not shown), were shown to have growth inhibitory activity against leukemia cells. 

Takeuehi et al. have synthesized biotin-labeled fostriecin (241), which possessed an inhibitory activity against the proliferation of mouse leukemia cells and demonstrated that the fostriecin covalently bound to the Cys269 residue of PP2Ac in HeLa S3 cells. ... 

Vlrazole, a -D-rlbofuranosyl derivative, has demonstrated a broad spectrum of in vitro inhibitory activity against adenovirus, HSV I and II, vaccinia, myxoma virus, parainfluenza, rhinovirus, Coxsackie virus and influenza A and B,91 it is more potent than other antl-lnfluenzal compounds in vitro and is effective against HSV keratitis and localized vaccinia. Friend leukemia virus, influenza A and parainfluenza I in vivo. The antiviral effect may be due to the inhibition of guanosine-T -phosphate synthesis in the infected cell. ... 

The aqueous extracts of U. tomentosa showed the significant inhibitory activity against human leukemia cancer ceU fines (K562 and HL 60) and a human EBV-transformed B l3mphoma ceU line. Literature revealed that the extract of this plant-induced apoptosis, in conjugation with DNA fragmentation, which evidences the antitumor activity [38,37], The aqueous extract of this plant had also been tested for toxicity against Chinese hamster ovary cells, which revealed that it is nontoxic at low concentrations [62],... 

---