Studies of in vitro anti-prostate cancer potential of newer 1,2,4-triazolo-1,3,4-thiadiazines with different heteroaromatics

Authors

  • Mao-Chuan Fan Department of Urology, The First Affiliated Hospital of Xinxiang Medical University, Henan 453100, China
  • Guang-Ye Han Department of Urology, The First Affiliated Hospital of Xinxiang Medical University, Henan 453100, China
  • Xin-Jun Zhang Department of Urology, The First Affiliated Hospital of Xinxiang Medical University, Henan 453100, China
  • Hui-Fang Xi Department of Pediatric Surgery, The First Affiliated Hospital of Xinxiang Medical University, Henan 453100, China

DOI:

https://doi.org/10.3329/bjp.v10i2.22424

Keywords:

Anti-cancer, Coumarin, Heterocycles, Prostate cancer

Abstract

This study was aimed to evaluate anticancer potential of newer synthesize 1,2,4-triazolo[3,4-b]-1,3,4-thiadiazines and its derivatives. All newly furnished scaffolds were subjected to screening for their in vitro anticancer potential against DU-145 and PC-3 prostate cancer cell lines using SRB and MMT bioassays. The structures of final compounds were confirmed with the aid of FT-IR, 1H NMR, 13C NMR spectroscopy and CHN analysis. Bioassay studies suggested that all thiadiazines were promising cytotoxic agents with % cytotoxicity ranging from 44.39-71.24%, whereas potent GI50 level in the range 11.96-32.51 µg/mL and results were comparable to the potencies of control drugs adriamycin and doxorubicin. Variation of heterocyclic pharmacophores along with the C-5 position of 1,2,4-triazole in terms of quinoline, quinazoline, coumarin and pyridine lead to the different SAR predictions in which quinoline and benzimidazole moieties found most promising.

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Additional Files

Published

2015-04-08

How to Cite

Fan, M.-C., G.-Y. Han, X.-J. Zhang, and H.-F. Xi. “Studies of in Vitro Anti-Prostate Cancer Potential of Newer 1,2,4-Triazolo-1,3,4-Thiadiazines With Different Heteroaromatics”. Bangladesh Journal of Pharmacology, vol. 10, no. 2, Apr. 2015, pp. 308-15, doi:10.3329/bjp.v10i2.22424.

Issue

Section

Research Articles