Synthesis, Computational Study, and Evaluation of In Vitro Antimicrobial, Antibiofilm, and Anticancer Activities of New Sulfanyl Aminonaphthoquinone Derivatives


Bayrak N., Yildirim H., Tuyun A. F., Kara E. M., Celik B. O., Gupta G. K., ...More

LETTERS IN DRUG DESIGN & DISCOVERY, vol.14, no.6, pp.647-661, 2017 (SCI-Expanded, Scopus)

  • Publication Type: Article / Article
  • Volume: 14 Issue: 6
  • Publication Date: 2017
  • Doi Number: 10.2174/1570180813666161020164931
  • Journal Name: LETTERS IN DRUG DESIGN & DISCOVERY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.647-661
  • Keywords: Naphthoquinones, aminoquinones, antibacterial activity, antifungal activity, antibiofilm activity, anticancer activity, NCI, colon cancer, docking study, NATIONAL-CANCER-INSTITUTE, 1,4-NAPHTHOQUINONE DERIVATIVES, BIOLOGICAL EVALUATION, CONTAINING HETERO-1,4-NAPHTHOQUINONES, SUBSTITUTED 1,4-NAPHTHOQUINONES, CHEMOSELECTIVE SYNTHESIS, CYTOTOXICITY EVALUATION, DRUG DISCOVERY, ANTIFUNGAL, ANTIBACTERIAL
  • Istanbul University Affiliated: Yes

Abstract

Background: A set of novel sulfanyl aminonaphthoquinone derivatives (5a-j) were synthesized starting from 2,3-dichloro-1,4-naphthoquinone (1). The amine substituents were introduced via a nucleophilic substitution at reflux temperature. Subsequent reactions of 2-chloro-3-arylamino-1,4-naphthoquinones (3a-d) with different thiols (4a-c) led to the formation of the desired amino-and thio-substituted products (5a-j).