Cell cycle effects of CB30865, a lipophilic quinazoline-based analogue of the antifolate thymidylate synthase inhibitor ICI 198583 with an undefined mechanism of action

Cytometry

Volumn 33, Issue 1, 1998, Pages 56-66

  Skelton, L A ^a   Ormerod, M G ^a   Titley, J C ^a   Jackman, A L ^a  

^a INSTITUTE OF CANCER RESEARCH   (United Kingdom)

Author keywords

Bromodeoxyuridine; CB30865; DNA histogram; Hoechst propidium iodide; Novel locus; Simultaneous arrest; Thymidylate synthase inhibitors

Indexed keywords

2 DEAMINO 2 METHYL 10 PROPARGYL 5,8 DIDEAZAFOLIC ACID; 4 [N (7 BROMO 3,4 DIHYDRO 2 METHYL 4 OXO 6 QUINAZOLINYLMETHYL) N (2 PROPYNYL)AMINO] N (3 PYRIDYLMETHYL)BENZAMIDE; FOLIC ACID ANTAGONIST; PYRIDINE DERIVATIVE; QUINAZOLINE DERIVATIVE; THYMIDYLATE SYNTHASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ANTINEOPLASTIC ACTIVITY; ARTICLE; CELL CYCLE; CONTROLLED STUDY; DNA DETERMINATION; DRUG MECHANISM; DRUG STRUCTURE; ENZYME INHIBITION; FLOW CYTOMETRY; HUMAN; HUMAN CELL; LEUKEMIA L 1210; MALIGNANT NEOPLASTIC DISEASE; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; BISBENZIMIDE; BROMODEOXYURIDINE; CELL CYCLE; CELL DIVISION; DNA, NEOPLASM; FLOW CYTOMETRY; FOLIC ACID; FOLIC ACID ANTAGONISTS; GROWTH INHIBITORS; HUMANS; MICE; PROPIDIUM; PYRIDINES; QUINAZOLINES; STAINING AND LABELING; THYMIDYLATE SYNTHASE; TUMOR CELLS, CULTURED;

ANIMALIA; MURINAE;

EID: 0032171607     PISSN: 01964763     EISSN: None     Source Type: Journal    
DOI: 10.1002/(SICI)1097-0320(19980901)33:1<56::AID-CYTO7>3.0.CO;2-9     Document Type: Article

References (15)

1. Charcosset JY: Effects of antineoplastic agents on the cell cycle progression. Biol Cell 58:135-138, 1986.
2. Grindey GB, Boder GB, Harper RW, Howbert JJ, Poore GA, Rieder BJ, Shaw WN, Todd CC, Worzalla JF: Identification of diarylsulfonylureas as novel antitumour agents. Proc Amer Assoc Cancer Res 28:277, 1986.
3. Marsham PR, Jackman AL, Barker AJ, Boyle FT, Pegg SJ, Wardleworth M, Kimbell R, O'Connor BM, Calvert AH, Hughes LR: Quinazoline antifolate thymidylate synthase inhibitors: Replacement of glutamic acid in the C2-methyl series. J Med Chem 38:994-1004, 1995.
4. Martin KJ, Chen SF, Clark GM, Degen D, Wajima M, Von Hoff DD, Kaddurah-Daouk R: Evaluation of creatine analogues as a new class of anticancer agents using freshly explanted human tumor cells. J Natl Cancer Inst 86:608-613, 1994.
5. Martin KJ, Winslow ER, Kaddurah-Daouk R: Cell cycle studies of cyclocreatine, a new anticancer agent. Cancer Res 34:5160-5165, 1994.
6. Ormerod MG: Analysis of DNA. General Methods. In: Flow Cytometry: A Practical Approach, 2nd Ed., Ormerod MG (ed). Oxford University Press, New York, 1994, pp. 118-135.
7. Ormerod MG, Kubbies M: Cell cycle analysis of asynchronous cell populations by flow cytometry using bromodeoxyuridine label and Hoechst-propidium iodide stain. Cytometry 13:678-685, 1992.
8. Rabinovitch PS, Kubbies M, Chen YC, Schindler D, Hoehn H: BrdU-Hoechst flow cytometry: A unique tool for quantitative cell cycle analysis. Exp Cell Res 174(2):309-318, 1988.
9. 3/c1 cells. Biochem Pharmacol 44:2387-2394, 1992.
10. Skelton LA, Kimbell R, Jackman AL: Aminomethyl pyridine analogues of the quinazoline antifolate ICI 198583 with a folate-independent locus of action. In: Chemistry and Biology of Pteridines and Folates, Pfleiderer W, Rokos H (eds). Blackwell Science, Berlin, 1997, pp. 209-212.
11. Skelton LA, Kimbell R, Kelland L, Ormerod MG, Titley J, Boyle FT, Jackman AL: Folate-based 3-pyridyl quinazolines of undefined mechanism of action as potential anti-tumour agents. Ann Oncol 7(Suppl 1):89, 1996.
12. Skelton LA, Kimbell R, Kelland L, Ormerod MG, Titley J, Jackman AL: Mechanistic studies with CB30865: A lipophilic quinazoline analogue of folic acid. Proc Amer Assoc Cancer Res 37:394, 1996.
13. Skelton LA, Ormerod MG, Boyle FT, Jackman AL: Unusual mechanism of action of a folate-based 3-pyridyl quinazoline. Cytometry Suppl 8:43, 1996.
14. Thakar JH, Chapin C, Berg RH, Ashmun RA, Houghton PJ: Effect of antitumour diarylsulfonylureas on in vivo and in vitro mitochondrial structure and function. Cancer Res 51:6286-6291, 1991.
15. Walliman T, Wyss M, Brdiczka D, Nicolay K, Eppenberger HM: Intracellular compartmentation, structure and function of creatine kinase isoenzymes in tissues with high fluctuating energy demands: The "phosphocreatine circuit" for cellular energy homeostasis. Biochem J 281:21-40, 1992.