Cytotoxic and anticancer activities of some 1-aryl-2-dimethylaminomethyl- 2-propen-1-one hydrochlorides

J. R. Dimmock, S. C. Vashishtha, S. A. Patil, N. Udupa, S. B. Dinesh, P. U. Devi, R. Kamath

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

A series of 1-aryl-2-dimethylaminomethyl-2-propen-1-one hydrochlorides demonstrated marked cytotoxicity towards approximately 55 human tumour cell lines from different neoplastic diseases. In general they were more potent than melphalan and displayed selective toxicity towards human leukemic cells. A representative compound, 1-phenyl-2-dimethylaminomethyl-2-propen-1-one hydrochloride (2a), had similar cytotoxicity as melphalan towards murine P388 and L1210 leukemic cells. In addition, 2a reduced the sizes of a number of human tumour xenografts including colon, prostatic and melanotic cancers passaged in athymic mice. Compound 2a showed excellent activity towards Ehrlich ascites carcinoma and B16F1 melanoma in mice which was enhanced using niosomes. One may conclude from the data generated that 1-aryl-2- dimethylaminomethyl-2-propen-1-one hydrochlorides are a novel series of cytotoxic and anticancer agents.

Original languageEnglish
Pages (from-to)702-706
Number of pages5
JournalPharmazie
Volume53
Issue number10
Publication statusPublished - 1998

Fingerprint

Melphalan
Cytotoxicity
Tumors
Cytotoxins
Heterografts
Liposomes
Antineoplastic Agents
Toxicity
Cells
Tumor Cell Line
Ascites
Nude Mice
Melanoma
Prostatic Neoplasms
Colon
Carcinoma
Neoplasms
2-dimethylaminomethyl-1-phenyl-2-propen-1-one

All Science Journal Classification (ASJC) codes

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science

Cite this

Dimmock, J. R., Vashishtha, S. C., Patil, S. A., Udupa, N., Dinesh, S. B., Devi, P. U., & Kamath, R. (1998). Cytotoxic and anticancer activities of some 1-aryl-2-dimethylaminomethyl- 2-propen-1-one hydrochlorides. Pharmazie, 53(10), 702-706.
Dimmock, J. R. ; Vashishtha, S. C. ; Patil, S. A. ; Udupa, N. ; Dinesh, S. B. ; Devi, P. U. ; Kamath, R. / Cytotoxic and anticancer activities of some 1-aryl-2-dimethylaminomethyl- 2-propen-1-one hydrochlorides. In: Pharmazie. 1998 ; Vol. 53, No. 10. pp. 702-706.
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Dimmock, JR, Vashishtha, SC, Patil, SA, Udupa, N, Dinesh, SB, Devi, PU & Kamath, R 1998, 'Cytotoxic and anticancer activities of some 1-aryl-2-dimethylaminomethyl- 2-propen-1-one hydrochlorides', Pharmazie, vol. 53, no. 10, pp. 702-706.

Cytotoxic and anticancer activities of some 1-aryl-2-dimethylaminomethyl- 2-propen-1-one hydrochlorides. / Dimmock, J. R.; Vashishtha, S. C.; Patil, S. A.; Udupa, N.; Dinesh, S. B.; Devi, P. U.; Kamath, R.

In: Pharmazie, Vol. 53, No. 10, 1998, p. 702-706.

Research output: Contribution to journalArticle

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AB - A series of 1-aryl-2-dimethylaminomethyl-2-propen-1-one hydrochlorides demonstrated marked cytotoxicity towards approximately 55 human tumour cell lines from different neoplastic diseases. In general they were more potent than melphalan and displayed selective toxicity towards human leukemic cells. A representative compound, 1-phenyl-2-dimethylaminomethyl-2-propen-1-one hydrochloride (2a), had similar cytotoxicity as melphalan towards murine P388 and L1210 leukemic cells. In addition, 2a reduced the sizes of a number of human tumour xenografts including colon, prostatic and melanotic cancers passaged in athymic mice. Compound 2a showed excellent activity towards Ehrlich ascites carcinoma and B16F1 melanoma in mice which was enhanced using niosomes. One may conclude from the data generated that 1-aryl-2- dimethylaminomethyl-2-propen-1-one hydrochlorides are a novel series of cytotoxic and anticancer agents.

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Dimmock JR, Vashishtha SC, Patil SA, Udupa N, Dinesh SB, Devi PU et al. Cytotoxic and anticancer activities of some 1-aryl-2-dimethylaminomethyl- 2-propen-1-one hydrochlorides. Pharmazie. 1998;53(10):702-706.