Nitric Oxide Releasing Derivatives of [(2-Chloroethyl)ureido] Benzoic Acid Esters as Potential Antineoplastic Agents

Hülya AKGÜN; Barkın BERK; Dilek Demir EROL

Article Details

Nitric Oxide Releasing Derivatives of [(2-Chloroethyl)ureido] Benzoic Acid Esters as Potential Antineoplastic Agents

Authors:

Hülya AKGÜN | Barkın BERK | Dilek Demir EROL

Publisher:

TUBITAK

Journal:

Turkish Journal of Chemistry 2009 Vol.33 Issue 1, pp.107-121

Document Type:

Article

Publication Date:

12/2008

Document Language:

Turkish

Document ID (Org No.):

2000728379

Frequency:

Bimonthly

eISSN:

1303-6130

pISSN:

1300-0527

Abstract:

 

New series of [(2-chloroethyl)ureido] benzoic acids  (compounds 3-8) and nitric oxide releasing derivatives of  [(2-chloroethyl)ureido] benzoic acid esters (compounds 9-14) were  synthesized as potential anti-cancer agents.  These compounds were  screened for their anti-proliferative activities on A549 (human lung  carcinoma) cells and for their cytotoxic effects on L929 (mouse  fibroblast) cells.  The compounds 3-8 exhibited mild cytotoxic effects  on L929 cells (cell viability from 100% to 85% -- 90% only) whereas  they had very little anti-proliferative activities towards A549 lung  carcinoma cells.  On the other hand, compounds 10, 11, and 13 had some  growth inhibition activity in A549 (human lung carcinoma) cells.  Among them, compounds 11 and 13 exhibited better anti-proliferative  activities towards A549 cells, but also appeared to be cytotoxic  towards L929 cells.  In this group, the compound 10 with  (1-(2-nitrooxyethyl)-3-[(2-chloroethyl)ureido]benzoate) structure  appeared to have very weak anti-neoplastic activity towards A549  cells, with very little cytotoxic activity towards fibroblasts at  physiological concentrations.  Therefore, this compound is a better  candidate for a potential anti-cancer therapy for non-small cell lung  carcinomas.  However, further studies are required in order to show  applicability and effectiveness in animal models for this type of  cancer.

 

New series of [(2-chloroethyl)ureido] benzoic acids  (compounds 3-8) and nitric oxide releasing derivatives of  [(2-chloroethyl)ureido] benzoic acid esters (compounds 9-14) were  synthesized as potential anti-cancer agents.  These compounds were  screened for their anti-proliferative activities on A549 (human lung  carcinoma) cells and for their cytotoxic effects on L929 (mouse  fibroblast) cells.  The compounds 3-8 exhibited mild cytotoxic effects  on L929 cells (cell viability from 100% to 85% -- 90% only) whereas  they had very little anti-proliferative activities towards A549 lung  carcinoma cells.  On the other hand, compounds 10, 11, and 13 had some  growth inhibition activity in A549 (human lung carcinoma) cells.  Among them, compounds 11 and 13 exhibited better anti-proliferative  activities towards A549 cells, but also appeared to be cytotoxic  towards L929 cells.  In this group, the compound 10 with  (1-(2-nitrooxyethyl)-3-[(2-chloroethyl)ureido]benzoate) structure  appeared to have very weak anti-neoplastic activity towards A549  cells, with very little cytotoxic activity towards fibroblasts at  physiological concentrations.  Therefore, this compound is a better  candidate for a potential anti-cancer therapy for non-small cell lung  carcinomas.  However, further studies are required in order to show  applicability and effectiveness in animal models for this type of  cancer.

Article Details

Nitric Oxide Releasing Derivatives of [(2-Chloroethyl)ureido] Benzoic Acid Esters as Potential Antineoplastic Agents

Authors: Hülya AKGÜN | Barkın BERK | Dilek Demir EROL

Publisher: TUBITAK

Journal: Turkish Journal of Chemistry 2009 Vol.33 Issue 1, pp.107-121

Document Type: Article

Publication Date: 12/2008

Document Language: Turkish

Document ID (Org No.): 2000728379

Frequency: Bimonthly

eISSN: 1303-6130

pISSN: 1300-0527

Issues

Authors:

Hülya AKGÜN | Barkın BERK | Dilek Demir EROL

Publisher:

TUBITAK

Journal:

Turkish Journal of Chemistry 2009 Vol.33 Issue 1, pp.107-121

Document Type:

Article

Publication Date:

12/2008

Document Language:

Turkish

Document ID (Org No.):

2000728379

Frequency:

Bimonthly

eISSN:

1303-6130

pISSN:

1300-0527