Bis - [2-(Chloroethyl) Amino] Acetamido - 4 - Substituted Phenyl Thiazole Derivatives As Possible Antioxidant And Alky-lating Anticancer Agents

Authors

  • Mahender Mohan Seth G. L. Bihani S. D. College of Technical Education (Pharmacy), Sri Ganganagar (Rajasthan) India.
  • V. Murugan Department of Pharmaceutical Chemistry, Dayananda Sagar College of Pharmacy, Kumaraswamy Layout, Bangalore, India.
  • Geetha K.M Department of Pharmaceutical Chemistry, Dayananda Sagar College of Pharmacy, Kumaraswamy Layout, Bangalore, India.
  • Mahesh Kumar Kataria Seth G. L. Bihani S. D. College of Technical Education (Pharmacy), Sri Ganganagar (Rajasthan) India.

Keywords:

Thiazole derivatives, nitrogen mustard, acetophenone, 2-amino-4-phenyl thiazole, MTT assay

Abstract

A series of new thiazole derivatives containing nitrogen mustard have been prepared by the cyclization with various substituted acetophenone with thiourea in presence of iodine to form 2-amino-4-phenyl thiazole. The 2-amino-4-phenyl thiazole acetylation with chloroacetylchloride was used to produce the corresponding 2-chloroacetamido-4-phenyl thiazoles. The resultant chloroacetyl derivatives were subjected to a nucleophilic substitution reaction with diethanolamine by heating under reflux in dry pyridine. The compounds thus obtained were subjected to chlorination reaction using phosphorous oxychloride to get title compounds. Compounds prepared were recrystallized from dimethyl sulphoxide. All the synthesized compounds were screened for their in-vitro cytotoxic activity by MTT assay, in-vivo anticancer activity against Dalton’s ascetic lymphoma (DAL) in Swiss albino mice and in-vitro anti-oxidant activity by 2’2- diphenyl-1-picryl hydrazyl and hydrogen peroxide scavenging methods.

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References

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Published

2018-03-01
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Mahender Mohan, V. Murugan, Geetha K.M, and Mahesh Kumar Kataria. “Bis - [2-(Chloroethyl) Amino] Acetamido - 4 - Substituted Phenyl Thiazole Derivatives As Possible Antioxidant And Alky-Lating Anticancer Agents”. International Journal of Pharmaceutics and Drug Analysis, vol. 6, no. 3, Mar. 2018, pp. 352-60, https://ijpda.com/index.php/journal/article/view/386.

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