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.

Downloads

Download data is not yet available.
Abstract
429
Download
288 Read
175

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